Cat. No.: HY-50767

Palbociclib

(Synonyms: PD 0332991)

245 Cited Publications

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Based on 245 publication(s) in Google Scholar

Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 571190-30-2
Formula: C₂₄H₂₉N₇O₂
Molecular Weight:447.53

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Palbociclib Chemical Structure

CAS No.: 571190-30-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (245)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target^[1]

Cdk4/cyclin D3

9 nM (IC₅₀)

Cdk4/cyclin D1

11 nM (IC₅₀)

Cdk6/cyclin D2

16 nM (IC₅₀)

DYRK1A

2000 nM (IC₅₀)

MAPK

8000 nM (IC₅₀)

CDK4

CCND1

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	0.032 μM Compound: Palbociclib	Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
A-375	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
A549	EC₅₀	0.4 μM Compound: Palbociclib	Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
A549	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
A549	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
A549	IC₅₀	1.32 μM Compound: V	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
A549	IC₅₀	8.07 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
A549	IC₅₀	9.4 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
B16-F10	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
BPH-1	GI₅₀	7.442 μM Compound: Palbociclib	Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
Calu-1	EC₅₀	33 μM Compound: Palbociclib	Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
COLO 205	IC₅₀	0.036 μM Compound: Palbociclib	Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
COLO 205	IC₅₀	300.6 nM Compound: Palbociclib	Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
CWR22R	GI₅₀	0.435 μM Compound: Palbociclib	Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
DU-145	GI₅₀	5.792 μM Compound: Palbociclib	Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
DU-145	IC₅₀	7.5 μM Compound: 31, PD-0332991	Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 24417566]
HCC38	EC₅₀	1.4 μM Compound: 51	Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
HCT-116	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
HCT-116	IC₅₀	7.11 μM Compound: 1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HCT-116	IC₅₀	8.9 μM Compound: V	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
HEK293	GI₅₀	9.608 μM Compound: Palbociclib	Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HeLa	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
HeLa	IC₅₀	13.3 μM Compound: 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HepG2	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
HepG2	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
HepG2	IC₅₀	9.92 μM Compound: Palbociclib	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
HL-60	GI₅₀	29.17 μM Compound: Palbociclib	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34958208]
HL-60	GI₅₀	3.498 μM Compound: Palbociclib	Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HT-29	IC₅₀	3.56 μM Compound: 1	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HT-29	IC₅₀	9.3 μM Compound: Palbociclib	Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
JeKo-1	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
Jurkat	GI₅₀	>100 μM Compound: Palbociclib	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
Jurkat	IC₅₀	1.495 μM Compound: Palbociclib	Anti-proliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Anti-proliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 38943626]
K562	GI₅₀	2.455 μM Compound: Palbociclib	Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
K562	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
K562	IC₅₀	2 μM Compound: 31, PD-0332991	Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 24417566]
L02	GI₅₀	>100 μM Compound: Palbociclib	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
L02	IC₅₀	25.63 μM Compound: Pal	Cytotoxicity against human L02 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
L02	IC₅₀	34.12 μM Compound: Pal	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
LNCaP C4-2B	GI₅₀	4.15 μM Compound: Palbociclib	Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MCF-10A	GI₅₀	19.07 μM Compound: Palbociclib	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	GI₅₀	>100 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MCF7	GI₅₀	0.557 μM Compound: Palbociclib	Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MCF7	GI₅₀	3.938 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
MCF7	IC₅₀	0.34 μM Compound: PD0332991	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MCF7	IC₅₀	0.78 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MCF7	IC₅₀	240 nM Compound: 1	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MCF7	IC₅₀	4.09 μM Compound: V	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MCF7	IC₅₀	5.81 μM Compound: Palbociclib	Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MCF7	IC₅₀	6.21 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay	[PMID: 38283222]
MCF7	IC₅₀	85.2 nM Compound: Palbociclib	Antiproliferative activity against Rb-proficient human MCF7 cells assessed as inhibition of cellular viability Antiproliferative activity against Rb-proficient human MCF7 cells assessed as inhibition of cellular viability	[PMID: 38670537]
MDA-MB-231	EC₅₀	0.3 μM Compound: 51	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
MDA-MB-231	GI₅₀	>100 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MDA-MB-231	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
MDA-MB-231	IC₅₀	14.6 μM Compound: Paldociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	3.5 μM Compound: V	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MDA-MB-231	IC₅₀	4.72 μM Compound: PD0332991	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MDA-MB-231	IC₅₀	5.22 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay	[PMID: 38283222]
MDA-MB-231	IC₅₀	5.62 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MDA-MB-231	IC₅₀	580 nM Compound: 1	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MDA-MB-231	IC₅₀	6.21 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
MDA-MB-435	IC₅₀	0.16 μM Compound: 43(table 3)	Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line	[PMID: 15801831]
MDA-MB-435	IC₅₀	160 nM Compound: PD-0332991	Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis	[PMID: 26115571]
MDA-MB-436	EC₅₀	5 μM Compound: 51	Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
MDA-MB-436	IC₅₀	>10000 nM Compound: Palbociclib	Antiproliferative activity against Rb-deficient human MDA-MB-436 cells assessed as inhibition of cellular viability Antiproliferative activity against Rb-deficient human MDA-MB-436 cells assessed as inhibition of cellular viability	[PMID: 38670537]
MDA-MB-453	GI₅₀	0.326 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay	[PMID: 28156111]
MDA-MB-453	IC₅₀	137 nM Compound: 1	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MDA-MB-453	IC₅₀	6.93 μM Compound: PD0332991	Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MDA-MB-468	EC₅₀	1.9 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
MDA-MB-468	GI₅₀	5.96 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MDA-MB-468	IC₅₀	>3 μM Compound: 43(table 3)	Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line	[PMID: 15801831]
MDA-MB-468	IC₅₀	>3 μM Compound: PD-0332991	Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis	[PMID: 26115571]
MDA-MB-468	IC₅₀	5424 nM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
MIA PaCa-2	IC₅₀	10.6 μM Compound: Palbociclib	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 33316409]
MM1.S	IC₅₀	200 nM Compound: PD	Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay	[PMID: 31330105]
MOLM-13	GI₅₀	>80 μM Compound: Palbociclib	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34958208]
MOLM-13	GI₅₀	0.062 μM Compound: Palbociclib	Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MOLM-13	IC₅₀	>3 μM Compound: Palbociclib	Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs	[PMID: 24641103]
MOLM-13	IC₅₀	0.011 μM Compound: Palbociclib	Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs	[PMID: 24641103]
MOLM-13	IC₅₀	0.096 μM Compound: Palbociclib	Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
MOLM-13	IC₅₀	0.096 μM Compound: Palbociclib	Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
MRC5	GI₅₀	>10 μM Compound: Palbociclib	Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MV4-11	GI₅₀	0.05 μM Compound: Palbociclib	Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay	[PMID: 28156111]
NB-4	GI₅₀	0.066 μM Compound: Palbociclib	Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
NCI-H1299	IC₅₀	0.27 μM Compound: Pal	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H1299	IC₅₀	0.31 μM Compound: Pal	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H1299	IC₅₀	8.92 μM Compound: PD0332991	Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
NCI-H2228	IC₅₀	1.42 μM Compound: Pal	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H2228	IC₅₀	1.62 μM Compound: Pal	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.22 μM Compound: Pal	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.22 μM Compound: Pal	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.26 μM Compound: Pal	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
OVCAR-3	IC₅₀	>3 μM Compound: 1	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay	[PMID: 34110834]
PC-3	GI₅₀	0.071 μM Compound: Palbociclib	Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
PC-3	IC₅₀	2.2 μM Compound: V	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
Raji	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
RPMI-8226	GI₅₀	2.215 μM Compound: Palbociclib	Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
Sf9	IC₅₀	>10 μM Compound: Palbociclib	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	>10 μM Compound: Palbociclib	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	>10 μM Compound: Palbociclib	Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	>100 μM Compound: Palbociclib	Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as	[PMID: 30665142]
Sf9	IC₅₀	>100 μM Compound: Palbociclib	Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	0.005 μM Compound: Palbociclib	Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.013 μM Compound: Palbociclib	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.013 μM Compound: Palbociclib	Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	1.1 μM Compound: Palbociclib	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	1.207 μM Compound: Palbociclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	8.75 μM Compound: Palbociclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	9.1 μM Compound: Palbociclib	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	9.2 μM Compound: PD-0332991	Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP	[PMID: 26851505]
Sf9	IC₅₀	9.8 μM Compound: Palbociclib	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
SK-MEL19	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T47D	EC₅₀	0.35 μM Compound: Palbociclib	Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
T47D	GI₅₀	1.056 μM Compound: Palbociclib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
U-266	GI₅₀	11.274 μM Compound: Palbociclib	Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
U-87MG ATCC	IC₅₀	345.2 nM Compound: Palbociclib	Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
U-937	IC₅₀	0.14 μM Compound: Palbociclib	Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
ZR-75-1	GI₅₀	2.279 μM Compound: Palbociclib	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]

In Vitro

Palbociclib (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser⁷⁹⁵ in MDA-MB-435 cells with an IC₅₀ value of 0.063 μM, and obtains similar effects on both Ser⁷⁸⁰ and Ser⁷⁹⁵ phosphorylation in the Colo-205 colon carcinoma^[1].
Palbociclib (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase^[1].
Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells^[2].
Palbociclib (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC₅₀ values ranging from 4 nM to 1 μM^[3].
Palbociclib (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC₅₀ values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-453 cells
Concentration:

0-1 μM
Incubation Time:

24 h
Result:

Arrested MDA-MB-453 cells in G1.

Cell Proliferation Assay^[3]

Cell Line:

ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
Concentration:

0-1 μM
Incubation Time:

6 days
Result:

Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

In Vivo

Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth^[1].
Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects^[2].
Palbociclib (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)^[1]
Dosage:

75, 150 mg/kg, daily for 14 days
Administration:

Oral adminstration
Result:

Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.

Animal Model:

Tumor-free female FVB mice^[2]
Dosage:

90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
Administration:

Oral adminstration
Result:

Reduced total thymic mass and immature CD4⁺ and CD8⁺ double-positive thymocytes, and increased the fractions of CD4⁺ and CD8⁺ single-positive thymocytes.

Animal Model:

Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)^[4]
Dosage:

100 mg/kg, daily for 1 week.
Administration:

Oral adminstration
Result:

Decreased the luminescence signal in liver and delayed tumour growth.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 571190-30-2
Appearance Solid
Molecular Weight 447.53
Formula C₂₄H₂₉N₇O₂
Color Light yellow to yellow
SMILES

O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C
Synonyms

PD 0332991
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (245)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Nature

Epigenetic therapy induces transcription of inverted SINEs and ADAR1 dependency. [Abstract]

2020 Dec;588(7836):169-173. PMID: 33087935
Nature

Fasting-mimicking diet and hormone therapy induce breast cancer regression. [Abstract]

2020 Jul;583(7817):620-624. PMID: 32669709
Nature

CDK4/6 inhibition triggers anti-tumour immunity. [Abstract]

2017 Aug 24;548(7668):471-475. PMID: 28813415
Nature

The metabolic function of cyclin D3-CDK6 kinase in cancer cell survival. [Abstract]

2017 Jun 15;546(7658):426-430. PMID: 28607489

Palbociclib purchased from MedChemExpress. Usage Cited in: Nature. 2017 Jun 15;546(7658):426-430. [Abstract]

In vitro kinase reactions using immunoprecipitated endogenous CDK6 and recombinant PFKP or PKM2 with or without Palbociclib (PALBO). ³²P-PFKP and ³²P-PKM2 denote phosphorylated proteins, IB, immunoblotting.
Cancer Cell

GABAergic neuronal lineage development determines clinically actionable targets in diffuse hemispheric glioma, H3G34-mutant. [Abstract]

2024 Aug 27:S1535-6108(24)00305-2. PMID: 39232581
Cancer Cell

Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]

2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026
Cancer Cell

Cell-Cycle-Targeting MicroRNAs as Therapeutic Tools against Refractory Cancers. [Abstract]

2017 Apr 10;31(4):576-590.e8. PMID: 28399412
Mol Cancer

Genome-wide in vivo CRISPR screen identifies TGFβ3 as actionable biomarker of palbociclib resistance in triple negative breast cancer. [Abstract]

2024 Jun 3;23(1):118. PMID: 38831405
Mol Cancer

S6K1 amplification confers innate resistance to CDK4/6 inhibitors through activating c-Myc pathway in patients with estrogen receptor-positive breast cancer. [Abstract]

2022 Aug 30;21(1):171. PMID: 36042494
Cancer Discov

NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]

2024 Sep 13:OF1-OF20. PMID: 39269178
Nat Methods

Efficient targeted insertion of large DNA fragments without DNA donors. [Abstract]

2022 Mar;19(3):331-340. PMID: 35228726
Nat Cancer

IL-17A-secreting γδ T cells promote resistance to CDK4/CDK6 inhibitors in HR+HER2- breast cancer via CX3CR1+ macrophages. [Abstract]

2025 Jul 7. PMID: 40624238
Nat Cancer

CDK4/6 inhibition reprograms the breast cancer enhancer landscape by stimulating AP-1 transcriptional activity. [Abstract]

2021 Jan;2(1):34-48. PMID: 33997789
Nat Immunol

Cell cycle arrest enhances CD8+ T cell effector function by potentiating glucose metabolism and IL-2 signaling. [Abstract]

2026 Mar;27(3):463-475. PMID: 41555086
Immunity

Mitochondrial DNA released by senescent tumor cells enhances PMN-MDSC-driven immunosuppression through the cGAS-STING pathway. [Abstract]

2025 Apr 8;58(4):811-825.e7. PMID: 40203808
Nat Cell Biol

Electrophilic compound screening identifies GPX4-dependent ferroptosis as a senescence vulnerability. [Abstract]

2026 May;28(5):915-929. PMID: 42032311
Nat Cell Biol

An SP110-SP100 axis is a critical regulator of promyelocytic leukaemia body dynamics and mitotic fidelity. [Abstract]

2026 Mar 13. PMID: 41826696
Mol Cell

CDK4/6 inhibitor-mediated cell overgrowth triggers osmotic and replication stress to promote senescence. [Abstract]

2023 Nov 16;83(22):4062-4077.e5. PMID: 37977118
Mol Cell

A fluorophore-conjugated reagent enabling rapid detection, isolation and live tracking of senescent cells. [Abstract]

2023 Oct 5;83(19):3558-3573.e7. PMID: 37802028
Cancer Res

Targeting transcriptional regulation with a CDK9 inhibitor suppresses growth of endocrine- and palbociclib-resistant ER+ breast cancers. [Abstract]

2024 Jan 2;84(1):17-25. PMID: 37801608
Cancer Res

Abemaciclib is effective in palbociclib-resistant hormone receptor-positive metastatic breast cancers. [Abstract]

2023 Oct 2;83(19):3264-3283. PMID: 37384539
Cancer Res

Kinome reprogramming is a targetable vulnerability in ESR1 fusion-driven breast cancer. [Abstract]

2023 Oct 2;83(19):3237-3251. PMID: 37071495

Palbociclib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2023 Oct 2;83(19):3237-3251. [Abstract]

Palbociclib (100 nM) inhibits cell growth in YFP control cells treated with E2 and ESR1-e6>YAP1, as well as in cells expressing ESR1-TAFs (SOX, ARNT2, and LPP) and two ERα LBD point mutants. The inhibitory effect on cells is significantly enhanced when combined with Pralsetinib (HY-112301) (500 nM).
Cancer Res

A Genome-Wide CRISPR Activation Screen Identifies PRRX2 as a Regulator of Enzalutamide Resistance in Prostate Cancer. [Abstract]

2022 Jun 6;82(11):2110-2123. PMID: 35405009
Cancer Res

Hormonal Regulation of Semaphorin 7a in ER+ Breast Cancer Drives Therapeutic Resistance. [Abstract]

2021 Jan 1;81(1):187-198. PMID: 33122307
Mol Cell

Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer. [Abstract]

2020 Jun 18;78(6):1096-1113.e8. PMID: 32416067
Cancer Res

CDK4 Regulates Lysosomal Function and mTORC1 Activation to Promote Cancer Cell Survival. [Abstract]

2019 Oct 15;79(20):5245-5259. PMID: 31395606
Mol Cell

CDK4 Phosphorylates AMPKα2 to Inhibit Its Activity and Repress Fatty Acid Oxidation. [Abstract]

2017 Oct 19;68(2):336-349.e6. PMID: 29053957
ACS Nano

Senescence-Primed Ferroptosis Enabled by a Metal-Organic Framework Nanoplatform for Enhanced Cancer Therapy. [Abstract]

2025 Dec 23;19(50):42689-42704. PMID: 41358603
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]

2026 Jan 22;17(1):619. PMID: 41571637
Nat Commun

O-GlcNAcylation of FOXK1 co-opts BAP1 to orchestrate the E2F pathway and promotes oncogenesis. [Abstract]

2025 Jul 1;16(1):5959. PMID: 40593803
Nat Commun

Attenuated growth factor signaling during cell death initiation sensitizes membranes towards peroxidation. [Abstract]

2025 Feb 25;16(1):1774. PMID: 40000627
Nat Commun

Hijacking of nucleotide biosynthesis and deamidation-mediated glycolysis by an oncogenic herpesvirus. [Abstract]

2024 Feb 16;15(1):1442. PMID: 38365882

Palbociclib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 16;15(1):1442. [Abstract]

Palbociclib (50 nM; 4 h) effectively blocks S1900 phosphorylation of CAD in both KSHV de novo-infected human oral keratinocytes (HOKs) and KSHV-positive BCBL-1 lymphoma cells.
Nat Commun

Oxidative phosphorylation is a metabolic vulnerability of endocrine therapy and palbociclib resistant metastatic breast cancers. [Abstract]

2023 Jul 14;14(1):4221. PMID: 37452026
Nat Commun

Targeting the Retinoblastoma/E2F repressive complex by CDK4/6 inhibitors amplifies oncolytic potency of an oncolytic adenovirus. [Abstract]

2022 Aug 10;13(1):4689. PMID: 35948546
Nat Commun

Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation. [Abstract]

2021 Nov 16;12(1):6607. PMID: 34785661
Nat Commun

Co-targeting CDK4/6 and AKT with endocrine therapy prevents progression in CDK4/6 inhibitor and endocrine therapy-resistant breast cancer. [Abstract]

2021 Aug 25;12(1):5112. PMID: 34433817

Palbociclib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

The efficacy of Fulvestrant (Fulv, 100 nM), CDK4/6 inhibitor (CDK4/6i) Palbociclib (Palbociclib isothiocyanate; 200 nM) and the dual PI3K/mTOR inhibitor (PI3K/mTORi) Gedatolisib (10 nM) as single agents or in double and triple combination, was assessed in M-S and MPF-R cells by crystal violet growth assay performed over 6 days.

Palbociclib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

The efficacy of Fulvestrant (Fulv, 100 nM), CDK4/6 inhibitor (CDK4/6i) Palbociclib (Palbociclib isothiocyanate; 200 nM) and the dual PI3K/mTOR inhibitor (PI3K/mTORi) Gedatolisib (10 nM) as single agents or in double and triple combination, was assessed in T-S and TPF-R cells by crystal violet growth assay performed over 6 days.

Palbociclib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

MPF-R and TPF-R cells were treated with different concentrations of the CDK4/6 inhibitor (CDK4/6i) Palbociclib (HY-A0065), Ribociclib (HY-15777C) or Abemaciclib (HY-16297A) for 6 days. Cell growth was measured by crystal violet colorimetric assay. Growth relative to vehicle (%) is plotted against log drug concentration.
Nat Commun

Oncogenic enhancers drive esophageal squamous cell carcinogenesis and metastasis. [Abstract]

2021 Jul 22;12(1):4457. PMID: 34294701
Nat Commun

PLK1 inhibition exhibits strong anti-tumoral activity in CCND1-driven breast cancer metastases with acquired palbociclib resistance. [Abstract]

2020 Aug 13;11(1):4053. PMID: 32792481
Nat Commun

Identification of predictors of drug sensitivity using patient-derived models of esophageal squamous cell carcinoma. [Abstract]

2019 Nov 7;10(1):5076. PMID: 31700061
Nat Commun

LEM4 confers tamoxifen resistance to breast cancer cells by activating cyclin D-CDK4/6-Rb and ERα pathway. [Abstract]

2018 Oct 9;9(1):4180. PMID: 30301939

Palbociclib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Oct 9;9(1):4180. [Abstract]

MCF7, MCF7-LEM4, and MCF7-TAMR cells are treated with 5% DCC-FBS (vehicle), 4-OHT (1 μM), PD0332991 (PD) (0.2 μM), or a combination of 4-OHT and PD0332991. Immunoblots of lysates from cells are tested.
Cell Death Differ

E2F and STAT3 provide transcriptional synergy for histone variant H2AZ activation to sustain glioblastoma chromatin accessibility and tumorigenicity. [Abstract]

2022 Jul;29(7):1379-1394. PMID: 35058574
Cell Death Differ

ARID1A prevents squamous cell carcinoma initiation and chemoresistance by antagonizing pRb/E2F1/c-Myc-mediated cancer stemness. [Abstract]

2020 Jun;27(6):1981-1997. PMID: 31831874
Neuron

Seeded aggregation of TDP-43 induces its loss of function and reveals early pathological signatures. [Abstract]

2025 Mar 26:S0896-6273(25)00180-1. PMID: 40157355
Trends Biotechnol

Long-offset paired nicking-based efficient and precise strategy for in vivo targeted insertion. [Abstract]

2025 Apr 7:S0167-7799(25)00083-6. PMID: 40199626
Sci Transl Med

Dual PI3K/mTOR inhibition is required to combat resistance to CDK4/6 inhibitor and endocrine therapy in PIK3CA-mutant breast cancer. [Abstract]

2025 Dec 17;17(829):eadp5088. PMID: 41406241

Palbociclib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

Combined Palbociclib- and Fulvestrant-resistant cells, M-S and T-S, and the corresponding resistant cells, MPF-R and TPF-R, were treated with different inhibitors of the PI3K/AKT/mTOR pathway including Alpelisib (HY-15244; Alp; 1 μM in M-S/MPF-R and 250 to 500 nM in T-S/TPF-R), Capivasertib (Cap; 250 to 500 nM in M-S/MPF-R and 100 nM in T-S/TPF-R), Sapanisertib (Sap; 10 nM in M-S/MPF-R and 5 nM in T-S/TPF-R), and Gedatolisib (HY-10681; Ged; 10 nM) in combination with Palbociclib (HY-50767; Palbo; 200 nM) and Fulvestrant (HY-13636; Fulv; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

Palbociclib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

Combined Palbociclib- and Fulvestrant-resistant cells (wild type ER+ breast cancer cells), ZPF-R, and the corresponding sensitive cells, Z-S, were treated with different inhibitors of PI3K/AKT/mTOR including Alpelisib (HY-15244; 6 μM), Capivasertib (50 nM), Sapanisertib (5 nM), and Gedatolisib (HY-10681; 5 nM) in combination with Palbociclib (HY-50767; 150 nM) and Fulvestrant (HY-13636; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

Palbociclib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

Triple combination with Gedatolisib (HY-10681), Palbociclib (HY-50767), and Fulvestrant (HY-13636) effectively inhibits growth of PIK3CA-mutant ER+ tumor xenografts resistant to combined palbociclib and fulvestrant. MPF-R cells (1 × 106) resistant to combined palbociclib and fulvestrant were injected into the mammary fat pads of NOG CIEA mice, and tumors were allowed to establish for 2 weeks to a size of ≈30 mm3. Mice were then treated with the combination of Fulvestrant (100 mg/kg, sc weekly), Palbociclib (25 mg/kg, oral gavage daily), and Capivasertib (100 mg/kg, oral gavage daily; n = 6) or Alpelisib (HY-15244; 25 mg/kg, oral gavage daily; n = 5). Tumor size was measured weekly. Average tumor growth curves measured weekly and Tumor volumes measured after excision.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

Biomimetic Nanomedicine for Senescence-Modulated Immune Activation Enhances Immunotherapy Efficacy in Hepatocellular Carcinoma. [Abstract]

2025 Dec 23:e17792. PMID: 41432006
Adv Sci (Weinh)

De Novo Gene Transcription of Connexin Mediates Cytoplasmic Fluid Exchange and Flocking Transitions in Physiological and Cancerous Epithelial Systems. [Abstract]

2025 Dec 23:e08648. PMID: 41431893
Adv Sci (Weinh)

CDK4/6 Inhibitors Impede Chemoresistance and Inhibit Tumor Growth of Small Cell Lung Cancer. [Abstract]

2024 Aug 13:e2400666. PMID: 39136283

Palbociclib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Aug 13:e2400666. [Abstract]

Palbociclib (PD) (0.5 µM; 24 h) induces the interaction between CDK6 and AMBRA1/CUL4A, but not LC3B, in H69AR cells.
J Clin Invest

Dual targeting CDK4/6 and CDK7 augments tumor response and anti-tumor immunity in breast cancer models. [Abstract]

2025 Aug 12:e188839. PMID: 40794455
Nucleic Acids Res

Rapid photo-crosslinking in living cells reveals protein-nucleic acid dynamics on a timescale of minutes. [Abstract]

2026 Apr 13;54(7):gkag339. PMID: 42011781
Nucleic Acids Res

PARP1 and PARP2 are dispensable for DNA repair by microhomology-mediated end-joining at double-ended DSBs. [Abstract]

2026 Jan 5;54(1):gkaf1437. PMID: 41495903
J Exp Clin Cancer Res

Integrated genomic analyses in PDX model reveal a cyclin-dependent kinase inhibitor Palbociclib as a novel candidate drug for nasopharyngeal carcinoma. [Abstract]

2018 Sep 20;37(1):233. PMID: 30236142

Palbociclib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 20;37(1):233. [Abstract]

Western blot of the nine cell cycle-related proteins in C666-1 cells treated with different concentrations of GEM (0.1, 1, and 10 μM) and PAL (0.1, 1, and 5 μM) after 48 h.
Sci Adv

Somatic CRISPR tumorigenesis and multiomic analysis reveal a pentose phosphate pathway disruption vulnerability in MPNSTs. [Abstract]

2025 Aug 15;11(33):eadu2906. PMID: 40802750
Mol Ther

CDK4/6 inhibition enhances CAR-T cell therapy in solid tumors. [Abstract]

2026 Mar 24:S1525-0016(26)00210-8. PMID: 41883164
Environ Sci Technol

Azocyclotin Binds CDK4 to Disrupt DNA Methylation in Zebrafish Epigenetic Transgenerational Inheritance. [Abstract]

2025 Dec 23;59(50):27130-27142. PMID: 41359812
EBioMedicine

Enhancer demethylation-regulated gene score identified molecular subtypes, inspiring immunotherapy or CDK4/6 inhibitor therapy in oesophageal squamous cell carcinoma. [Abstract]

2024 Jul:105:105177. PMID: 38924839
EBioMedicine

MYC status as a determinant of synergistic response to Olaparib and Palbociclib in ovarian cancer. [Abstract]

2019 May:43:225-237. PMID: 30898650

Palbociclib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 May:43:225-237. [Abstract]

Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with AZD2281 and Palbociclib either as single-agents or in combination for 4 days.
EBioMedicine

Potent anti-tumor efficacy of palbociclib in treatment-naïve H3.3K27M-mutant diffuse intrinsic pontine glioma. [Abstract]

2019 May:43:171-179. PMID: 31060906
MedComm (2020)

In vivo visualization of fluorescence reflecting CDK4 activity in a breast cancer mouse model. [Abstract]

2022 Jun 10;3(3):e136. PMID: 35711853
Cell Rep Med

CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]

2025 Dec 29:102526. PMID: 41468895
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Clin Cancer Res

ESR1 Y537S and D538G mutations drive resistance to CDK4/6 inhibitors in estrogen receptor-positive breast cancer. [Abstract]

2025 May 1;31(9):1667-1675. PMID: 39992682
Clin Cancer Res

CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]

2024 Sep 13;30(18):4179-4189. PMID: 39052240
Clin Cancer Res

Radiotherapy Delivered before CDK4/6 Inhibitors Mediates Superior Therapeutic Effects in ER+ Breast Cancer. [Abstract]

2021 Apr 1;27(7):1855-1863. PMID: 33495311

Palbociclib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2021 Apr 1;27(7):1855-1863. [Abstract]

Palbociclib (100-500 nM) significantly inhibits cell growth in MCF7 cells and demonstrates a robust additive cytostatic effect when administered 6 hours post-radiotherapy.
Cancer Lett

A NIR-Ⅱ fluorescent probe for real-time visualization and early assessment of responses to CDK4/6 inhibitors in breast cancer. [Abstract]

2026 May 28:646:218429. PMID: 41825845
Cancer Lett

PI3K inhibitor idelalisib enhances the anti-tumor effects of CDK4/6 inhibitor palbociclib via PLK1 in B-cell lymphoma. [Abstract]

2024 May 28:216996. PMID: 38815797
Int J Biol Sci

Transcription Factor E2F4 Promote Proliferation, Migration, and Invasion of Gastric Cancer Cells by transcriptionally activating DSCC1. [Abstract]

2024 Sep 16;20(12):4978-4998. PMID: 39309429
Int J Biol Sci

The G1 phase optical reporter serves as a sensor of CDK4/6 inhibition in vivo. [Abstract]

2021 Jan 31;17(3):728-741. PMID: 33767584
Int J Biol Sci

Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. [Abstract]

2019 Jan 1;15(3):522-532. PMID: 30745839
Acta Biomater

Tissue-adhesive hydrogel for multimodal drug release to immune cells in skin. [Abstract]

2022 Sep 15:150:211-220. PMID: 35921992
Cell Death Dis

The RBPJ/DAPK3/UBE3A signaling axis induces PBRM1 degradation to modulate the sensitivity of renal cell carcinoma to CDK4/6 inhibitors. [Abstract]

2022 Apr 2;13(4):295. PMID: 35368029
Cell Death Dis

c-myc regulates the sensitivity of breast cancer cells to palbociclib via c-myc/miR-29b-3p/CDK6 axis. [Abstract]

2020 Sep 15;11(9):760. PMID: 32934206
Cell Death Dis

Pan-cancer analysis reveals synergistic effects of CDK4/6i and PARPi combination treatment in RB-proficient and RB-deficient breast cancer cells. [Abstract]

2020 Apr 6;11(4):219. PMID: 32249776
Proc Natl Acad Sci U S A

RPA-independent activation of the ATR/CHK1 pathway. [Abstract]

2026 Feb 10;123(6):e2524246123. PMID: 41628322
Dev Cell

Palbociclib releases the latent differentiation capacity of neuroblastoma cells. [Abstract]

2023 Oct 9;58(19):1967-1982.e8. PMID: 37734383

Palbociclib purchased from MedChemExpress. Usage Cited in: Dev Cell. 2023 Oct 9;58(19):1967-1982.e8. [Abstract]

Palbociclib (PB) (1 μM; 24 h) reduces RB phosphorylation in SK-N-BE(2)C, IMR-32, and SH-SY5Y cells.

Palbociclib purchased from MedChemExpress. Usage Cited in: Dev Cell. 2023 Oct 9;58(19):1967-1982.e8. [Abstract]

Palbociclib (PB) (1 μM; 5 days) significantly reduces proliferation in SK-N-BE(2)C, IMR-32, and SH-SY5Y cells.
(B–D) Representative fluorescent images of EdU incorporation following a 24-h pulse in (B) SK-N-BE(2)C, (C) IMR-32, and (D) SH-SY5Y cells (pulse began day 4 of 5-day treatment with vehicle [DMSO] or palbociclib [1 μM]). Scale bars: 100 μm. Analysis of % cells with EdU incorporation. n = 3 biological replicates, mean ± SEM. ∗∗p ≤ 0.01, one-tailed paired t test. DAPI nuclear counters
EMBO Mol Med

Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML. [Abstract]

2025 Aug 29. PMID: 40883610
EMBO J

CEP192 localises mitotic Aurora-A activity by priming its interaction with TPX2. [Abstract]

2024 Nov;43(22):5381-5420. PMID: 39327527
EMBO J

Mouse models to investigate in situ cell fate decisions induced by p53. [Abstract]

2024 Oct;43(19):4406-4436. PMID: 39160273
Phytomedicine

Hernandezine acts as a CDK4 suppressor inhibiting tumor growth by the CDK4/PKM2/NRF2 axis in colon cancer. [Abstract]

2024 May 28:131:155775. PMID: 38838401
EMBO J

RNA sensing via the RIG-I-like receptor LGP2 is essential for the induction of a type I IFN response in ADAR1 deficiency. [Abstract]

2022 Mar 15;41(6):e109760. PMID: 35156720
EMBO J

USP7 limits CDK1 activity throughout the cell cycle. [Abstract]

2021 Jun 1;40(11):e99692. PMID: 33856059
NPJ Precis Oncol

IL-6 predicts CDK4/6 inhibitor resistance, identifying STAT3 as a target in HR + /HER2-negative metastatic breast cancer. [Abstract]

2025 Jul 25;9(1):260. PMID: 40715551
NPJ Precis Oncol

Acetylation of ELF5 suppresses breast cancer progression by promoting its degradation and targeting CCND1. [Abstract]

2021 Mar 19;5(1):20. PMID: 33742100
Neoplasia

The antitumor activity of osimertinib plus palbociclib in non-small cell lung cancer patient-derived xenograft (PDX)/2D/3D culture models harboring EGFR amplification and CDKN2A/2B homozygous deletions. [Abstract]

2024 Aug 14:57:101039. PMID: 39146623
Cell Syst

A Multi-center Study on the Reproducibility of Drug-Response Assays in Mammalian Cell Lines. [Abstract]

2019 Jul 24;9(1):35-48.e5. PMID: 31302153
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Neoplasia

Combined Inhibition of ATR and WEE1 as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. [Abstract]

2018 Mar 28;20(5):478-488. PMID: 29605721
NPJ Breast Cancer

JAK/STAT1-interferon-ISGylation networks in breast cancer resistance to inhibitors of FOXM1 and CDK4/6. [Abstract]

2026 Feb 12. PMID: 41680190
NPJ Breast Cancer

CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]

2025 Dec 3;11(1):135. PMID: 41339342
NPJ Breast Cancer

Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries. [Abstract]

2025 Nov 12;11(1):125. PMID: 41224743
NPJ Breast Cancer

MCM3 upregulation confers endocrine resistance in breast cancer and is a predictive marker of diminished tamoxifen benefit. [Abstract]

2021 Jan 4;7(1):2. PMID: 33398005
Biomed Pharmacother

A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma. [Abstract]

2025 Aug:189:118340. PMID: 40651458
JHEP Rep

Loss of Cdkn1a protects against MASLD alone or with alcohol intake by preserving lipid homeostasis. [Abstract]

2024 Oct 5;7(1):101230. PMID: 39659733
J Transl Med

Cellular senescence in the response of HR+ breast cancer to radiotherapy and CDK4/6 inhibitors. [Abstract]

2023 Feb 10;21(1):110. PMID: 36765430
J Transl Med

CDK4/6 inhibitor palbociclib suppresses IgE-mediated mast cell activation. [Abstract]

2019 Aug 20;17(1):276. PMID: 31429774
Cell Mol Gastroenterol Hepatol

Additive Effect of CD73 Inhibitor in Colorectal Cancer Treatment With CDK4/6 Inhibitor Through Regulation of PD-L1. [Abstract]

2022;14(4):769-788. PMID: 35843546
Oncogene

RB loss determines selective resistance and novel vulnerabilities in ER-positive breast cancer models. [Abstract]

2022 Jul;41(27):3524-3538. PMID: 35676324
Cell Chem Biol

CDK2 heterobifunctional degraders co-degrade CDK2 and cyclin E resulting in efficacy in CCNE1-amplified and overexpressed cancers. [Abstract]

2025 Apr 17;32(4):556-569.e24. PMID: 40250405
Cell Chem Biol

Multiomics Profiling Establishes the Polypharmacology of FDA-Approved CDK4/6 Inhibitors and the Potential for Differential Clinical Activity. [Abstract]

2019 Aug 15;26(8):1067-1080.e8. PMID: 31178407
Cell Chem Biol

Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. [Abstract]

2018 Feb 15;25(2):135-142.e5. PMID: 29276047
Aging Cell

Dynamic regulation of myofibroblast phenotype in cellular senescence. [Abstract]

2022 Apr;21(4):e13580. PMID: 35266275
Eur J Cancer

Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ataxia telangiectasia-mutated kinase-mediated DNA damage response. [Abstract]

2018 Oct:102:10-22. PMID: 30103095

Palbociclib purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Oct:102:10-22. [Abstract]

Head-to-head comparison of the effect of Palbociclib and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.
Cell Death Discov

CDK4/6 inhibition initiates cell cycle arrest by nuclear translocation of RB and induces a multistep molecular response. [Abstract]

2024 Oct 26;10(1):453. PMID: 39461947
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Cell Rep

Targeting protein tyrosine phosphatases for CDK6-induced immunotherapy resistance. [Abstract]

2023 Mar 30;42(4):112314. PMID: 37000627
Cell Rep

POLθ processes ssDNA gaps and promotes replication fork progression in BRCA1-deficient cells. [Abstract]

2022 Nov 29;41(9):111716. PMID: 36400033
Cell Rep

S-palmitoylation of PCSK9 induces sorafenib resistance in liver cancer by activating the PI3K/AKT pathway. [Abstract]

2022 Aug 16;40(7):111194. PMID: 35977495
Cell Rep

CDK/cyclin dependencies define extreme cancer cell-cycle heterogeneity and collateral vulnerabilities. [Abstract]

2022 Mar 1;38(9):110448. PMID: 35235778
Cell Rep

Disentangling Pro-mitotic Signaling during Cell Cycle Progression using Time-Resolved Single-Cell Imaging. [Abstract]

2020 Apr 14;31(2):107514. PMID: 32294432
Cell Rep

MicroRNA-Mediated Suppression of the TGF-β Pathway Confers Transmissible and Reversible CDK4/6 Inhibitor Resistance. [Abstract]

2019 Mar 5;26(10):2667-2680.e7. PMID: 30840889
Br J Cancer

Transiently hypoxic tumour cell turnover and radiation sensitivity in human tumour xenografts. [Abstract]

2022 Jun;126(11):1616-1626. PMID: 35031765
J Med Chem

Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase-1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation. [Abstract]

2021 Nov 11;64(21):15702-15715. PMID: 34670362
J Med Chem

3 H-Pyrazolo[4,3- f]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo. [Abstract]

2021 Aug 12;64(15):10981-10996. PMID: 34288692
Br J Cancer

RON signalling promotes therapeutic resistance in ESR1 mutant breast cancer. [Abstract]

2021 Jan;124(1):191-206. PMID: 33257837
Anal Chem

Minimally Invasive Single-Cell Metabolomics Analysis to Unveil Different Trajectories of Individual Cells in Ferroptosis. [Abstract]

2026 Mar 24;98(11):8133-8142. PMID: 41814887
EMBO Rep

CDK inhibitor Palbociclib targets STING to alleviate autoinflammation. [Abstract]

2022 Jun 7;23(6):e53932. PMID: 35403787
Ecotoxicol Environ Saf

PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]

2025 Nov 15:307:119433. PMID: 41273832
Mol Ther Nucleic Acids

Development of new non-viral systems for genetic modification of senescent cells. [Abstract]

2023 Mar 21:32:302-317. PMID: 37096164
JCI Insight

The CRTC1-MAML2 fusion is the major oncogenic driver in mucoepidermoid carcinoma. [Abstract]

2021 Apr 8;6(7):e139497. PMID: 33830080
Ecotoxicol Environ Saf

Cadmium inhibits apoptosis of human esophageal epithelial cells by upregulating CDK6. [Abstract]

2020 Dec 1;205:111146. PMID: 32827965
Cancer Cell Int

Organoids as a model system for researching human neuroendocrine tumor of the breast. [Abstract]

2024 Dec 27;24(1):433. PMID: 39731167
Int J Mol Med

MicroRNA‑885‑5p regulates cell cycle progression in liver cancer cells. [Abstract]

2025 Nov;56(5):167. PMID: 40808344
Breast Cancer Res

Lasofoxifene as a potential treatment for aromatase inhibitor-resistant ER-positive breast cancer. [Abstract]

2024 Jun 7;26(1):95. PMID: 38849889
Cell Prolif

PFKFB4 facilitates palbociclib resistance in oestrogen receptor-positive breast cancer by enhancing stemness. [Abstract]

2023 Jan;56(1):e13337. PMID: 36127291
Biochem Pharmacol

Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. [Abstract]

2017 Jan 15:124:29-42. PMID: 27816545
Mol Cancer Ther

Harnessing senolytics and PARP inhibition to expand the antitumor activity of CDK4/6 inhibitors in prostate cancer. [Abstract]

2025 Jul 2. PMID: 40601842
Inflamm Res

Cuproptosis-related gene CDKN2A as a molecular target for IPF diagnosis and therapeutics. [Abstract]

2023 Jun;72(6):1147-1160. PMID: 37166466
Mar Drugs

A Marine Alkaloid, Ascomylactam A, Suppresses Lung Tumorigenesis via Inducing Cell Cycle G1/S Arrest through ROS/Akt/Rb Pathway. [Abstract]

2020 Sep 27;18(10):494. PMID: 32992455
Liver Int

Epigenetic Regulation of MicroRNA Expression by Hepatitis B Virus Pre-S2 Mutant Promotes Hepatocellular Carcinoma Tumorigenesis. [Abstract]

2026 Apr;46(4):e70582. PMID: 41797438
Cells

Characterization of a Preclinical In Vitro Model Derived from a SMARCA4-Mutated Sinonasal Teratocarcinosarcoma. [Abstract]

2023 Dec 30;13(1):81. PMID: 38201285
J Pathol

Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]

2023 Jun;260(2):203-221. PMID: 36825655
Commun Biol

RBAP48 facilitates the oral squamous cell carcinoma process in an androgen receptor-dependent and independent manners. [Abstract]

2025 May 30;8(1):829. PMID: 40442479
Life Sci

CDK4/6 are necessary for UCP1-mediated thermogenesis of white adipose tissue. [Abstract]

2023 Jun 1:322:121652. PMID: 37011871

Palbociclib purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121652. [Abstract]

Palbociclib (1 µM; 48 h) decreases the expression of PPARγ in SVFs.
Int J Mol Sci

MYCN Amplification, along with Wild-Type RB1 Expression, Enhances CDK4/6 Inhibitors' Efficacy in Neuroblastoma Cells. [Abstract]

2023 Mar 12;24(6):5408. PMID: 36982482
Int J Mol Sci

Therapeutic Potential for Regulation of the Nuclear Factor Kappa-B Transcription Factor p65 to Prevent Cellular Senescence and Activation of Pro-Inflammatory in Mesenchymal Stem Cells. [Abstract]

2021 Mar 25;22(7):3367. PMID: 33805981
Int J Mol Sci

Cisplatin Synergistically Enhances Antitumor Potency of Conditionally Replicating Adenovirus via p53 Dependent or Independent Pathways in Human Lung Carcinoma. [Abstract]

2019 Mar 5;20(5). pii: E1125. PMID: 30841620
Biomolecules

Targeting Cellular Senescence to Enhance Human Endometrial Stromal Cell Decidualization and Inhibit Their Migration. [Abstract]

2025 Jun 16;15(6):873. PMID: 40563513
Mol Cancer Res

Dual Inhibition of CDK4 and CDK2 via Targeting p27 Tyrosine Phosphorylation Induces a Potent and Durable Response in Breast Cancer Cells. [Abstract]

2018 Mar;16(3):361-377. PMID: 29330290
Molecules

Inhibition of Mitochondrial Antioxidant Defense and CDK4/6 in Mesothelioma. [Abstract]

2023 May 27;28(11):4380. PMID: 37298855
Mol Oncol

Dinaciclib synergizes with BH3 mimetics targeting BCL-2 and BCL-XL in multiple myeloma cell lines partially-dependent on MCL-1 and in plasma cells from patients. [Abstract]

2023 Dec;17(12):2507-2525. PMID: 37704591
Mol Oncol

Palbociclib induces activation of AMPK and inhibits hepatocellular carcinoma in a CDK4/6-independent manner. [Abstract]

2017 Aug;11(8):1035-1049. PMID: 28453226

Palbociclib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]

Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

Palbociclib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]

Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

Palbociclib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]

Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.
Cancers (Basel)

Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]

2024 Aug 7;16(16):2785. PMID: 39199558
Cancers (Basel)

Stromal Senescence following Treatment with the CDK4/6 Inhibitor Palbociclib Alters the Lung Metastatic Niche and Increases Metastasis of Drug-Resistant Mammary Cancer Cells. [Abstract]

2023 Mar 22;15(6):1908. PMID: 36980794
Cancers (Basel)

Musashi1 Contribution to Glioblastoma Development via Regulation of a Network of DNA Replication, Cell Cycle and Division Genes. [Abstract]

2021 Mar 24;13(7):1494. PMID: 33804958
Cancers

Targeting Pharmacokinetic Drug Resistance in Acute Myeloid Leukemia Cells with CDK4/6 Inhibitors. [Abstract]

2020 Jun 16;12(6):1596. PMID: 32560251
Front Cell Dev Biol

FBXO2 Promotes Proliferation of Endometrial Cancer by Ubiquitin-Mediated Degradation of FBN1 in the Regulation of the Cell Cycle and the Autophagy Pathway. [Abstract]

2020 Aug 31;8:843. PMID: 32984335
J Cell Mol Med

Bortezomib suppresses self-renewal and leukemogenesis of leukemia stem cell by NF-ĸB-dependent inhibition of CDK6 in MLL-rearranged myeloid leukemia. [Abstract]

2021 Mar;25(6):3124-3135. PMID: 33599085
Transl Oncol

TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]

2025 Jan 3:52:102264. PMID: 39756156
iScience

Multiomic characterization and drug testing establish circulating tumor cells as an ex vivo tool for personalized medicine. [Abstract]

2022 Sep 6;25(10):105081. PMID: 36204272
J Cell Physiol

ELF4/TRIB3/CDK6 Axis Promotes Cancer Stem Cell Activity in Endometrial Cancer. [Abstract]

2025 Nov;240(11):e70113. PMID: 41287970
J Biol Chem

The E3 ligase β-TRCP1 earmarks OTUD3 for destruction to fine-tune cGAS activation. [Abstract]

2026 Jun;302(6):111461. PMID: 41999888
Sci Rep

Ganoderma lucidum spore oil with Ganoderma lucidum and Ganoderma sinense extracts (G2SO) shows antitumor and Immunomodulatory effects in mice. [Abstract]

2026 Jan 5;16(1):4751. PMID: 41491024
Sci Rep

Hybrid framework for lesion-aware, clinically coherent chest X-ray report generation using contrastive learning and large language models. [Abstract]

2026 Jan 5;16(1):4645. PMID: 41492086
Sci Rep

Dual-drug codelivery gelatin-based hydrogel of ARV-471 and Palbociclib enhances synergistic effect in breast cancer treatment. [Abstract]

2025 Nov 29. PMID: 41318792
Sci Rep

Steroid hormone receptors, exome sequencing and treatment responsiveness of breast cancer patient-derived xenografts originated in a South American country. [Abstract]

2025 Jan 18;15(1):2415. PMID: 39827242
J Biol Chem

Targeting the mitotic kinase NEK2 enhances CDK4/6 inhibitor efficacy by potentiating genome instability. [Abstract]

2025 Jan 16:108196. PMID: 39826695
J Biol Chem

Downregulation of the splicing regulator NSRP1 confers resistance to CDK4/6 inhibitors via activation of interferon signaling in breast cancer. [Abstract]

2024 Dec 10:108070. PMID: 39667501
Sci Rep

Selective but not pan-CDK inhibition abrogates 5-FU-driven tissue factor upregulation in colon cancer. [Abstract]

2024 May 8;14(1):10582. PMID: 38719932
J Biol Chem

Cyclin D1 extensively reprograms metabolism to support biosynthetic pathways in hepatocytes. [Abstract]

2023 Dec;299(12):105407. PMID: 38152849
J Biol Chem

The adapter protein FADD provides an alternate pathway for entry into the cell cycle by regulating APC/C-Cdh1 E3 ubiquitin ligase activity. [Abstract]

2023 Jun;299(6):104786. PMID: 37146968
Sci Rep

RNA disruption is a widespread phenomenon associated with stress-induced cell death in tumour cells. [Abstract]

2023 Jan 31;13(1):1711. PMID: 36720913
Sci Rep

Pre-therapeutic efficacy of the CDK inhibitor dinaciclib in medulloblastoma cells. [Abstract]

2021 Mar 8;11(1):5374. PMID: 33686114
J Virol

Targeting Cell Cycle Facilitates E1A-Independent Adenoviral Replication. [Abstract]

2023 Jun 29;97(6):e0037023. PMID: 37219458
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Cell Signal

MYC amplification sensitizes TNBC to CHK1 inhibitors. [Abstract]

2025 Jul:131:111709. PMID: 40037423
Biochim Biophys Acta

Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81. [Abstract]

2017 Nov 20;1865(2):354-363. PMID: 29157894

Palbociclib purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]

LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.
Development

Dysfunction of programmed embryo senescence is linked to genetic developmental defects. [Abstract]

2023 May 1;150(9):dev200903. PMID: 37017267
J Bone Oncol

Identification of GPC3 mutation and upregulation in a multidrug resistant osteosarcoma and its spheroids as therapeutic target. [Abstract]

2021 Sep 20:30:100391. PMID: 34611509
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Future Med Chem

Discovery of CDK4 inhibitors by convolutional neural networks. [Abstract]

2019 Feb;11(3):165-177. PMID: 30556417
Endocrinology

TRβ Agonism Induces Tumor Suppression and Enhances Drug Efficacy in Anaplastic Thyroid Cancer in Female Mice. [Abstract]

2023 Aug 28;164(10):bqad135. PMID: 37702560
Front Oncol

CDK6 Immunophenotype Implicates Potential Therapeutic Application of CDK4/6 Inhibitors in Urothelial Carcinoma. [Abstract]

2022 Apr 8;12:819003. PMID: 35463324
Discov Oncol

Mucinous breast cancer organoids: an in vitro research model. [Abstract]

2025 May 19;16(1):814. PMID: 40388071
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

The role of palbociclib on the alterations in CDKN2, CCNE1, E2F3, MDM2 expressions as target genes of miR-141. [Abstract]

2024 Aug 8;19(8):e0306545. PMID: 39116089
PLoS One

Quercetin inhibits the epithelial-mesenchymal transition and reverses CDK4/6 inhibitor resistance in breast cancer by regulating circHIAT1/miR-19a-3p/CADM2 axis. [Abstract]

2024 Jul 11;19(7):e0305612. PMID: 38990915
Cell Biochem Biophys

Mechanistic Regulation of Epidermal Growth Factor and Hormonal Receptors by Kinase Inhibitors and Organofluorines in Breast Cancer Therapy. [Abstract]

2025 Mar;83(1):1113-1137. PMID: 39316263
GEN Biotechnol

2025 Apr 17.
Biochem Biophys Res Commun

Polyphyllin I enhances the anti-tumor efficacy of Palbociclib by reversing M2 macrophage polarization in lung cancer. [Abstract]

2025 Jun 18:777:152228. PMID: 40578288
Biochem Biophys Res Commun

Glyoxalase 1 inhibitor BBGC suppresses the progression of chronic lymphocytic leukemia and promotes the efficacy of Palbociclib. [Abstract]

2023 Apr 2:650:96-102. PMID: 36774689
Leuk Res

Targeting cyclin-dependent kinases 4/6 inhibits survival of megakaryoblasts in acute megakaryoblastic leukaemia. [Abstract]

2022 Sep:120:106920. PMID: 35872339
Am J Transl Res

PIK3CA mutations contribute to fulvestrant resistance in ER-positive breast cancer. [Abstract]

2019 Sep 15;11(9):6055-6065. PMID: 31632573
bioRxiv

Disrupted Mitochondrial Copper Homeostasis Promotes Ferroptotic Stress, Senescence and MASLD Progression. [Abstract]

2026 Jun 17:2026.06.15.731916. PMID: 42367918
bioRxiv

2026 Apr 19.
bioRxiv

2026 Mar 13.
Charles University

2026.
bioRxiv

2026 Jan 25.
bioRxiv

Distinct p21 dynamics drive alternative routes to whole-genome duplication through a common CDK4/6-dependent polyploid G0 state. [Abstract]

2026 Jan 15:2026.01.15.699545. PMID: 41648389
bioRxiv

53BP1 condensates function as bioreactors for NHEJ directed DNA repair and insulators to determine pathway choice. [Abstract]

2025 Dec 23:2025.12.19.695596. PMID: 41509350
Res Sq

2025 Dec 18.
Technical University of Dresden

2025.
bioRxiv

2025 Dec 7.
bioRxiv

2025 Dec 14.
bioRxiv

A functional map of CDK-drug interactions at single amino acid resolution. [Abstract]

2025 Nov 3:2025.11.02.685764. PMID: 41279360
Technical University of Munich

2025.
bioRxiv

Mitotic bypass and endocycling promote cancer cell survival after genotoxic chemotherapy. [Abstract]

2025 Nov 4:2025.11.03.686258. PMID: 41278999
SSRN

2025 Oct 15.
bioRxiv

2025 Sep 15.
bioRxiv

2025 Aug 30.
SSRN

2025 Aug 14.
bioRxiv

2025 August 24.
University of Jena

2025.
Technische Universitat Darmstadt

2025 May 8.
bioRxiv

2025 May 10.
bioRxiv

2025 March 06.
Patent

US20240307414A1.
bioRxiv

CENcyclopedia: Dynamic Landscape of Kinetochore Architecture Throughout the Cell Cycle. [Abstract]

2024 Dec 5:2024.12.05.627000. PMID: 39677682
Research Square Preprint

2024 Nov 06.
bioRxiv

Therapeutic benefits of maintaining CDK4/6 inhibitors and incorporating CDK2 inhibitors beyond progression in breast cancer. [Abstract]

2024 Nov 15:2024.11.11.623139. PMID: 39605351

Palbociclib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Nov 15:2024.11.11.623139. [Abstract]

Continuous Palbociclib (1 μM) and fulvestrant (500 nM) treatment for 20 days significantly reduced resistant-cell growth compared to palbociclib discontinuation, fulvestrant alone, or fulvestrant plus INX-315 (100 nM).
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
Texas Southern University

2024 July 02.
bioRxiv

The molecular chronology of mammary epithelial cell fate switching. [Abstract]

2024 Nov 4:2024.10.08.617155. PMID: 39415993
bioRxiv

2024 July 05.
Res Sq

2024 Jun 04.
Research Square Preprint

2023 Nov 30.
bioRxiv

2023 Nov 23.
bioRxiv

Nanoparticle delivery of innate immune agonists combines with senescence-inducing agents to mediate T cell control of pancreatic cancer. [Abstract]

2023 Sep 18:2023.09.18.558307. PMID: 37790484
bioRxiv

CDK6-mediated endothelial cell cycle acceleration drives arteriovenous malformations in hereditary hemorrhagic telangiectasia. [Abstract]

2023 Sep 16:2023.09.15.554413. PMID: 37745444
Patent

US11761044.
World J Surg Surgical Res

2023 Jun 28.
Research Square Preprint

2023 May 9.
Patent

US20230149350A1.
Syddansk Universitet

2023 May 22.
bioRxiv

2023 Mar 30.
bioRxiv

2023 Mar 15.
University of Dundee

2023 Jan.
University College Dublin

2022.
University College Dublin

2022.
SSRN

2022 Nov 21.
Technischen Universität München

2022.
J Oncol

Palbociclib Enhances Migration and Invasion of Cancer Cells via Senescence-Associated Secretory Phenotype-Related CCL5 in Non-Small-Cell Lung Cancer. [Abstract]

2022 Sep 27:2022:2260625. PMID: 37181790
University of Coruña

2022 Oct.
University of Coruña

2022 Jan.
Research Square Preprint

2021 Dec.
Laurentian University

2021 Oct.
University of Texas

2021 Sep.
Technischen Universität Dresden

11 June 2021.
Research Square Preprint

2021 Apr.
Department of Biochemistry

2020 Oct.
Patent

US20200108066A1
Practical Oncology Journal

2018,32(03):193-197.
PRACTICAL ONCOLOGY JOURNAL

2018, 32(3): 193-197.

Solvent & Solubility

In Vitro:

0.1 M HCl : 25 mg/mL (55.86 mM; ultrasonic and warming and heat to 60°C)

DMSO : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 5 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2345 mL

11.1724 mL

22.3449 mL

5 mM

0.4469 mL

2.2345 mL

4.4690 mL

10 mM

0.2234 mL

1.1172 mL

2.2345 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Portuguese - PT (623 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Content Brief]

[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [Content Brief]

[3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. [Content Brief]

[4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / 0.1 M HCl	1 mM	2.2345 mL	11.1724 mL	22.3449 mL	55.8622 mL
	5 mM	0.4469 mL	2.2345 mL	4.4690 mL	11.1724 mL
	10 mM	0.2234 mL	1.1172 mL	2.2345 mL	5.5862 mL
0.1 M HCl	15 mM	0.1490 mL	0.7448 mL	1.4897 mL	3.7241 mL
	20 mM	0.1117 mL	0.5586 mL	1.1172 mL	2.7931 mL
	25 mM	0.0894 mL	0.4469 mL	0.8938 mL	2.2345 mL
	30 mM	0.0745 mL	0.3724 mL	0.7448 mL	1.8621 mL
	40 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	50 mM	0.0447 mL	0.2234 mL	0.4469 mL	1.1172 mL

Keywords

Palbociclib

245 Cited Publications

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Palbociclib

Peptidomimetic Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Palbociclib

All CDK Isoforms

Biological Activity

Chemical Information

Publications (245)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Palbociclib

Peptidomimetic Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Palbociclib

All CDK Isoforms

Biological Activity

Chemical Information

Publications (245)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Palbociclib Related Classifications

Cat. No.: HY-50767