Referencia número: HY-15777

Ribociclib

(Synonyms: LEE011)

84 Cited Publications

Revisión del cliente

Based on 84 publication(s) in Google Scholar

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.94%
No. CAS: 1211441-98-3
Fòrmula: C₂₃H₃₀N₈O
Peso molecular:434.54

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Ribociclib Chemical Structure

No. CAS: 1211441-98-3

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (84)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

CDK4

10 nM (IC₅₀)

CDK6

39 nM (IC₅₀)

Ver todos los productos específicos de isoformas CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
A-375	IC₅₀	>10 μM Compound: 1; RIB	Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33256948]
A549	IC₅₀	>10000 nM Compound: LEE011	Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
A549	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
A549	IC₅₀	7.455 μM Compound: Ribociclib	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
B16-F10	IC₅₀	>10 μM Compound: 1; RIB	Cytotoxicity against mouse B16F10 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against mouse B16F10 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33256948]
BJ	EC₅₀	>65.5172 μM Compound: 5	Antiproliferative activity against human BJ cells after 72 hrs by CelTiter-Glo assay Antiproliferative activity against human BJ cells after 72 hrs by CelTiter-Glo assay	[PMID: 29407975]
BXPC-3	IC₅₀	68.37 μM Compound: 1	Antiproliferative activity against human BxPC-3 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as inhibition of cell growth by MTT assay	[PMID: 33316409]
CCRF-CEM	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
HCC827	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human HCC827 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human HCC827 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
HeLa	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
Hep 3B2	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against human Hep3B cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human Hep3B cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
Hep 3B2	IC₅₀	9.264 μM Compound: Ribociclib	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
HepG2	EC₅₀	0.2862 μM Compound: 5	Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay	[PMID: 29407975]
HepG2	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
HepG2	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
Jurkat	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
KOPN-8	EC₅₀	0.5008 μM Compound: 5	Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay	[PMID: 29407975]
MCF7	IC₅₀	>10000 nM Compound: LEE011	Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
MCF7	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
MCF7	IC₅₀	48.66 μM Compound: Ribociclib	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]
MDA-MB-231	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
MDA-MB-231	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
MDA-MB-231	IC₅₀	27.3 μM Compound: Ribociclib	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	49.51 μM Compound: Ribociclib	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-468	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
MIA PaCa-2	IC₅₀	10.7 μM Compound: 1	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]
NCI-H1299	IC₅₀	7637 nM Compound: LEE011	Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
NCI-H1299	IC₅₀	5.46 μM Compound: Ribociclib	Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
NCI-H1299	IC₅₀	2.349 μM Compound: Ribociclib	Antiproliferative activity against human H1299 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human H1299 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
NCI-H1975	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
NCI-H460	IC₅₀	>10000 nM Compound: LEE011	Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
NCI-H460	IC₅₀	>10 μM Compound: Ribociclib	Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
PC-9	IC₅₀	5.342 μM Compound: Ribociclib	Antiproliferative activity against human PC9 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human PC9 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
SEM	EC₅₀	0.4605 μM Compound: 5	Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay	[PMID: 29407975]
Sf9	IC₅₀	>20 μM Compound: Ribociclib	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	>20 μM Compound: Ribociclib	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	>20 μM Compound: Ribociclib	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]
Sf9	IC₅₀	>20 μM Compound: Ribociclib	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	0.03 μM Compound: Ribociclib	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	3.9 μM Compound: Ribociclib	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]
SiHa	IC₅₀	>10 μM Compound: Ribociclib	Antiproliferative activity against human SiHa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human SiHa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
SUP-B15	EC₅₀	>65.5172 μM Compound: 5	Antiproliferative activity against human SUP-B15 cells after 72 hrs by CelTiter-Glo assay Antiproliferative activity against human SUP-B15 cells after 72 hrs by CelTiter-Glo assay	[PMID: 29407975]
T47D	IC₅₀	6227 nM Compound: LEE011	Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
T47D	IC₅₀	6.23 μM Compound: Ribociclib	Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 29518312]
U-937	IC₅₀	6.517 μM Compound: Ribociclib	Antiproliferative activity against human U937 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human U937 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
UoC-B1	EC₅₀	>65.5172 μM Compound: 5	Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay	[PMID: 29407975]

In Vitro

Ribociclib (500 nM; 6 days) inhibits the growth of neuroblastoma cell lines BE2C and IMR5^[2].

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

Western Blot Analysis^[2]

Cell Line:

Neuroblastoma cell lines BE2C and IMR5
Concentration:

10 nM、100 nM、250 nM、500 nM、750 nM、1 μM and 5 μM
Incubation Time:

6 days
Result:

Down-regulated FOXM1 protein expression level.

In Vivo

Ribociclib (200 mg/kg; p.o.; 21 days) delays tumor growth in CB17-immunodeficient BE2C or 1643 xenograft mice^[2].

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

Animal Model:

CB17 immunodeficient BE2C or 1643 xenograft mice^[2]
Dosage:

200 mg/kg
Administration:

p.o.; Once a day for 21 days
Result:

Reduced RB phosphorylation significantly.

Ensayo clínico

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

Chemical Information

No. CAS 1211441-98-3
Appearance Solid
Peso molecular 434.54
Fòrmula C₂₃H₃₀N₈O
Color Off-white to yellow
SMILES

O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5
Synonyms

LEE011
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (84)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayWB

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Journal Impact Factor

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
Cell

RNA Pol II inhibition activates cell death independently from the loss of transcription. [Abstract]

2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455
Cell

Rapid adaptation to CDK2 inhibition exposes intrinsic cell-cycle plasticity. [Abstract]

2023 Jun 8;186(12):2628-2643.e21. PMID: 37267950
Cancer Discov

INX-315, a selective CDK2 inhibitor, induces cell cycle arrest and senescence in solid tumors. [Abstract]

2024 Mar 1;14(3):446-467. PMID: 38047585
Nat Cancer

Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. [Abstract]

2021 Apr;2(4):429-443. PMID: 34568836
Mil Med Res

Expression dynamics of periodic transcripts during cancer cell cycle progression and their correlation with anticancer drug sensitivity. [Abstract]

2022 Dec 19;9(1):71. PMID: 36529792
Cancer Res

Profiling the Activity of the Potent and Highly Selective CDK2 Inhibitor BLU-222 Reveals Determinants of Response in CCNE1-Aberrant Ovarian and Endometrial Tumors. [Abstract]

2025 Apr 3;85(7):1297-1309. PMID: 39945650
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
Nat Commun

Induced pluripotent stem cell-derived models of malignant nerve sheath tumor progression mimic glial to neuro-mesenchymal transition and uncover therapeutic opportunities. [Abstract]

2026 Jun 17;17(1):5361. PMID: 42310314
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

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

Inhibition of CK1ε potentiates the therapeutic efficacy of CDK4/6 inhibitor in breast cancer. [Abstract]

2021 Sep 10;12(1):5386. PMID: 34508104

Ribociclib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Sep 10;12(1):5386. [Abstract]

D4476 (150 mg/kg; i.g.; daily). Combination of D4476 with Ribociclib (100 mg/kg; i.g.; daily) retards MDA-MB-231 tumor growth in vivo.
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

Ribociclib 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

Death effector domain-containing protein induces vulnerability to cell cycle inhibition in triple-negative breast cancer. [Abstract]

2019 Jun 28;10(1):2860. PMID: 31253784
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
Sci Adv

ACTR5 controls CDKN2A and tumor progression in an INO80-independent manner. [Abstract]

2022 Dec 23;8(51):eadc8911. PMID: 36563143
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

Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity. [Abstract]

2023 Oct 17;4(10):101200. PMID: 37734378
Clin Cancer Res

Triple Combination of MEK, BET, and CDK Inhibitors Significantly Reduces Human Malignant Peripheral Nerve Sheath Tumors in Mouse Models. [Abstract]

2025 Mar 3;31(5):907-920. PMID: 39786423
Clin Cancer Res

CDK4 Amplification Reduces Sensitivity to CDK4/6 Inhibition in Fusion-Positive Rhabdomyosarcoma. [Abstract]

2015 Nov 1;21(21):4947-59. PMID: 25810375

Ribociclib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]

Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.

Ribociclib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]

Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.
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
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
Cell Death Dis

CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells. [Abstract]

2020 Sep 15;11(9):754. PMID: 32934219
Int J Biol Macromol

CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609. [Abstract]

2024 Dec 27:139117. PMID: 39733900
NPJ Precis Oncol

Optimized culturing yields high success rates and preserves molecular heterogeneity, enabling personalized screening for high-grade gliomas. [Abstract]

2025 May 27;9(1):156. PMID: 40425813
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
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
J Transl Med

Personalized medicine strategy for MPNSTs: using precision oncology on PDOX models to inform tumor boards. [Abstract]

2026 Feb 4;24(1):385. PMID: 41639724
J Transl Med

CDK4/6 inhibitors sensitize gammaherpesvirus-infected tumor cells to T-cell killing by enhancing expression of immune surface molecules. [Abstract]

2022 May 13;20(1):217. PMID: 35562811
Biomed Pharmacother

Ribociclib, a selective cyclin D kinase 4/6 inhibitor, inhibits proliferation and induces apoptosis of human cervical cancer in vitro and in vivo. [Abstract]

2019 Apr:112:108602. PMID: 30784916
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
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

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

Head-to-head comparison of the effect of PD 0332991 and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.
Cell Rep

A Switch in p53 Dynamics Marks Cells That Escape from DSB-Induced Cell Cycle Arrest. [Abstract]

2020 Aug 4;32(5):107995. PMID: 32755587
Cell Rep

Differential Regulation of G1 CDK Complexes by the Hsp90-Cdc37 Chaperone System. [Abstract]

2017 Oct 31;21(5):1386-1398. PMID: 29091774
JCI Insight

RB expression confers sensitivity to CDK4/6 inhibitor-mediated radiosensitization across breast cancer subtypes. [Abstract]

2022 Feb 8;7(3):e154402. PMID: 34932500
Int J Mol Med

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

2025 Nov;56(5):167. PMID: 40808344
Biochem Pharmacol

Direct reprogramming of human fibroblasts into hair-inducing dermal papilla cell-like cells by a single small molecule. [Abstract]

2025 Jan 9:116744. PMID: 39798934
Breast Cancer Res

Estrogen receptor coregulator binding modulator (ERX-11) enhances the activity of CDK4/6 inhibitors against estrogen receptor-positive breast cancers. [Abstract]

2019 Dec 26;21(1):150. PMID: 31878959
Pharmaceutics

A Dual-Payload Bispecific ADC Improved Potency and Efficacy over Single-Payload Bispecific ADCs. [Abstract]

2025 Jul 25;17(8):967. PMID: 40870990
Mol Cancer Ther

Preclinical Activity of Abemaciclib Alone or in Combination with Antimitotic and Targeted Therapies in Breast Cancer. [Abstract]

2018 May;17(5):897-907. PMID: 29483214
Cells

Machine Learning-Driven Multi-Omics Analysis Identifies CHP2 as a Key PANoptosis-Related Dual-Function Biomarker in Colorectal Cancer. [Abstract]

2026 Feb 28;15(5):430. PMID: 41827864
Eur J Pharmacol

VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]

2025 Sep 15:1003:177942. PMID: 40651787
RSC Adv

2020, 10(38):22668-22683.
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Artif Cells Nanomed Biotechnol

Ribociclib (LEE011) suppresses cell proliferation and induces apoptosis of MDA-MB-231 by inhibiting CDK4/6-cyclin D-Rb-E2F pathway. [Abstract]

2019 Dec;47(1):4001-4011. PMID: 31588803
J Infect Dis

Ebola Virus VP40 Modulates Cell Cycle and Biogenesis of Extracellular Vesicles. [Abstract]

2018 Nov 22;218(suppl_5):S365-S387. PMID: 30169850
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

Ribociclib 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.

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

Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM for 72 h.
Cancers (Basel)

Combined Targeting of Pathogenetic Mechanisms in Pancreatic Neuroendocrine Tumors Elicits Synergistic Antitumor Effects. [Abstract]

2022 Nov 8;14(22):5481. PMID: 36428573
Cancers

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

2020 Jun 16;12(6):1596. PMID: 32560251
Transl Oncol

Radiosensitizing effects of CDK4/6 inhibitors in hormone receptor-positive and HER2-negative breast cancer mediated downregulation of DNA repair mechanism and NF-κB-signaling pathway. [Abstract]

2024 Aug 16:49:102092. PMID: 39153367
Sci Rep

Amplification of CDK4 and MDM2: a detailed study of a high-risk neuroblastoma subgroup. [Abstract]

2022 Jul 20;12(1):12420. PMID: 35859155
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
Front Oncol

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

2022 Apr 8;12:819003. PMID: 35463324
Naunyn Schmiedebergs Arch Pharmacol

Piperazine ring toxicity in three novel anti-breast cancer drugs: an in silico and in vitro metabolic bioactivation approach using olaparib as a case study. [Abstract]

2023 Jul;396(7):1435-1450. PMID: 36738368
J Pharm Biomed Anal

Identification and structural characterization of potential degraded impurities of ribociclib by time of flight -tandem mass spectrometry, and their toxicity prediction. [Abstract]

2021 Apr 15:197:113933. PMID: 33588298
J Chromatogr B Analyt Technol Biomed Life Sci

Time of flight mass spectrometry based in vitro and in vivo metabolite profiling of ribociclib and their toxicity prediction. [Abstract]

2020 Jun 15;1147:122142. PMID: 32416594
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 effect of ribociclib on the expression levels of miR-141 and CDK4/6-USP51 signaling pathway genes in MCF-7 and MDA-MB-231 cells. [Abstract]

2024 Aug 28;19(8):e0309289. PMID: 39196911
PLoS One

Combination of androgen receptor inhibitor enzalutamide with the CDK4/6 inhibitor ribociclib in triple negative breast cancer cells. [Abstract]

2022 Dec 22;17(12):e0279522. PMID: 36548336
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Biomed Res Int

Inhibition of the CDK4/6-Cyclin D-Rb Pathway by Ribociclib Augments Chemotherapy and Immunotherapy in Renal Cell Carcinoma. [Abstract]

2020 Jun 11;2020:9525207. PMID: 32626773
Leuk Res

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

2022 Sep:120:106920. PMID: 35872339
Biomed Chromatogr

Metabolic profiles of ribociclib in rat and human liver microsomes using liquid chromatography combined with electrospray ionization high-resolution mass spectrometry. [Abstract]

2020 Mar;34(3):e4783. PMID: 31899811
bioRxiv

2026 Jun 25.
bioRxiv

CDK4/6 inhibition sensitizes breast cancer to NK cell therapy by inducing immune-interactive surface proteins. [Abstract]

2026 Apr 22:2026.04.19.719504. PMID: 42079201
bioRxiv

2026 Jan 25.
Res Sq

2025 Dec 18.
bioRxiv

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

2025 Nov 3:2025.11.02.685764. PMID: 41279360
University of Innsbruck

2025.
bioRxiv

2025 Sep 15.
University of Jena

2025.
bioRxiv

2025 February 23.
Texas Southern University

2024 July 02.
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
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

US20220354911A1.
Research Square Print

November 7th, 2022
Department of Biochemistry

2020 Oct.

Solvente y solubilidad

In Vitro:

DMSO : 6.25 mg/mL (14.38 mM; Need ultrasonic; 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

2.3013 mL

11.5064 mL

23.0128 mL

5 mM

0.4603 mL

2.3013 mL

4.6026 mL

10 mM

0.2301 mL

1.1506 mL

2.3013 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 1 mg/mL (2.30 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC-Na/1% Tween-80 in Saline water

Solubility: 10 mg/mL (23.01 mM); Suspended solution; Need ultrasonic

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. [Content Brief]

[2]. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. [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

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3013 mL	11.5064 mL	23.0128 mL	57.5321 mL
	5 mM	0.4603 mL	2.3013 mL	4.6026 mL	11.5064 mL
	10 mM	0.2301 mL	1.1506 mL	2.3013 mL	5.7532 mL

Keywords

Ribociclib

84 Cited Publications

100 mg Obtener un presupuesto

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Ribociclib

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

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Orally Active Compound Library

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Protein Kinase Compound Library

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High-Throughput Bioactive Compound Library

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Posttranslational Modification Library

FDA Kinase Inhibitor Library

High-Efficiency Gene Editing Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Ribociclib

Ver todos los productos específicos de isoformas CDK

Actividad biológica

Chemical Information

Publications (84)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Ribociclib Related Classifications

HY-15777 Related Classifications