Art. -Nr.: HY-16297A

Abemaciclib

Name: Abemaciclib
Brand: MedChemExpress
SKU: HY-16297A
Price: 60.00 USD
Availability: InStock
Rating: 5 (129 reviews)

(Synonyms: LY2835219)

129 Cited Publications

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Based on 129 publication(s) in Google Scholar

Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

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Reinheit : 99.97%
CAS. Nr.: 1231929-97-7
Formel: C₂₇H₃₂F₂N₈
Molecular Weight:506.59

Speicherung:

4°C, protect from light

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

Abemaciclib Chemical Structure

CAS. Nr.: 1231929-97-7

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (129)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
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Bioz

Biologische Aktivität

Beschreibung

Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

IC₅₀ & Target

^[3]

Cdk4/cyclin D1

2 nM (IC₅₀)

CDK6/cyclinD1

10 nM (IC₅₀)

CDK9/cyclinT1

57 nM (IC₅₀)

CDK5/p35

287 nM (IC₅₀)

Cdk5/p25

355 nM (IC₅₀)

CDK2/cyclinE

504 nM (IC₅₀)

CDK1/cyclinB1

1627 nM (IC₅₀)

CDK7/Mat1/cyclinH1

3910 nM (IC₅₀)

PIM1

50 nM (IC₅₀)

PIM2

3400 nM (IC₅₀)

HIPK2

31 nM (IC₅₀)

DYRK2

61 nM (IC₅₀)

CK2

117 nM (IC₅₀)

GSK3b

192 nM (IC₅₀)

JNK3

389 nM (IC₅₀)

FLT3 (D835Y)

403 nM (IC₅₀)

DRAK1

659 nM (IC₅₀)

FLT3

3960 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A 172	EC₅₀	0.2 μM Compound: 3	Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
A549	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
BT-474	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human BT-474 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human BT-474 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
BXPC-3	IC₅₀	127 nM Compound: Abemaciclib	Antiproliferative activity against human BxPC3 cells Antiproliferative activity against human BxPC3 cells	[PMID: 31200237]
Calu-6	IC₅₀	17400 nM Compound: Chemical Probe: LY2835219	Cell cycle arrest in human Calu-6 cells assessed as reduction in pHH1 expression measured after 24 hrs by laser-scanning fluorescence cytometry Cell cycle arrest in human Calu-6 cells assessed as reduction in pHH1 expression measured after 24 hrs by laser-scanning fluorescence cytometry	[PMID: 24919854]
CFPAC-1	IC₅₀	371 nM Compound: Abemaciclib	Antiproliferative activity against human CFPAC-1 cells Antiproliferative activity against human CFPAC-1 cells	[PMID: 31200237]
COLO 205	EC₅₀	72 nM Compound: Chemical Probe: LY2835219	Cell cycle arrest in human COLO 205 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 24 hrs by propidium iodide staining based laser-scanning fluorescence cytometry Cell cycle arrest in human COLO 205 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 24 hrs by propidium iodide staining based laser-scanning fluorescence cytometry	[PMID: 24919854]
COLO 205	IC₅₀	0.217 μM Compound: Abemaciclib	Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay	[PMID: 29459274]
COLO 205	IC₅₀	0.46 μM Compound: LY2835219	Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay	[PMID: 29074254]
COLO 205	IC₅₀	120 nM Compound: LY-2835219	Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis	[PMID: 26115571]
COLO 205	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
COLO 205	IC₅₀	253 nM Compound: Abemaciclib	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	0.348 μM Compound: Abemaciclib	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]
DBTRG-05MG	EC₅₀	0.19 μM Compound: 3	Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
EMT6	IC₅₀	4.18 μM Compound: Abemaciclib	Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
HEK293	GI₅₀	10.925 μM Compound: Abemaciclib	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	768 nM Compound: Abemaciclib	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
HepG2	IC₅₀	216 nM Compound: Abemaciclib	Antiproliferative activity against human HepG2 cells Antiproliferative activity against human HepG2 cells	[PMID: 31200237]
HL-60	GI₅₀	0.664 μM Compound: Abemaciclib	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-22	IC₅₀	12.2 μM Compound: 1	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
HUVEC	IC₅₀	403 nM Compound: Abemaciclib	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
Jurkat	GI₅₀	4.63 μM Compound: Abemaciclib	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]
K562	GI₅₀	0.624 μM Compound: Abemaciclib	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	1090 nM Compound: Abemaciclib	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 31200237]
LNCaP	IC₅₀	84 nM Compound: Abemaciclib	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 31200237]
M059J	EC₅₀	9.24 μM Compound: 3	Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
MCF-10A	GI₅₀	5.088 μM Compound: Abemaciclib	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	0.832 μM Compound: Abemaciclib	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	GI₅₀	4.01 μM Compound: Abemaciclib	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	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human MCF7 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human MCF7 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
MCF7	IC₅₀	153 nM Compound: Abemacidib	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]
MCF7	IC₅₀	7.29 μM Compound: Abemaciclib	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	99.8 nM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
MDA-MB-231	GI₅₀	3.45 μM Compound: Abemaciclib	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	IC₅₀	>20 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
MDA-MB-231	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
MDA-MB-231	IC₅₀	18.58 μM Compound: Abemaciclib	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	191 nM Compound: LY2835219	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay	[PMID: 29429832]
MDA-MB-231	IC₅₀	62 nM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
MDA-MB-361	EC₅₀	20 nM Compound: Chemical Probe: LY2835219	Cell cycle arrest in human MDA-MB-361 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 6 days by propidium iodide staining based laser-scanning fluorescence cytometry Cell cycle arrest in human MDA-MB-361 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 6 days by propidium iodide staining based laser-scanning fluorescence cytometry	[PMID: 24919854]
MDA-MB-361	IC₅₀	90 nM Compound: Chemical Probe: LY2835219	Cytotoxicity against human MDA-MB-361 cells assessed as reduction in cell viability measured after 6 days Cytotoxicity against human MDA-MB-361 cells assessed as reduction in cell viability measured after 6 days	[PMID: 24919854]
MDA-MB-436	IC₅₀	1351 nM Compound: Abemacidib	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-468	IC₅₀	>20 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
MDA-MB-468	IC₅₀	1144 nM Compound: Abemaciclib	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]
MDA-MB-468	IC₅₀	4.808 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay	[PMID: 29459274]
MIA PaCa-2	IC₅₀	5.8 μM Compound: Abemaciclib	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-H1975	IC₅₀	774 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-H1975 cells Antiproliferative activity against human NCI-H1975 cells	[PMID: 31200237]
NCI-H1993	IC₅₀	1156 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-H1993 cells Antiproliferative activity against human NCI-H1993 cells	[PMID: 31200237]
NCI-H358	IC₅₀	80.7 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-H358 cells Antiproliferative activity against human NCI-H358 cells	[PMID: 31200237]
NCI-H441	IC₅₀	263 nM Compound: Abemaciclib	Antiproliferative activity against human H441 cells Antiproliferative activity against human H441 cells	[PMID: 31200237]
NCI-N87	IC₅₀	519 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-N87 cells Antiproliferative activity against human NCI-N87 cells	[PMID: 31200237]
Non-small cell lung cancer cell line	IC₅₀	0.7 μM Compound: 109	Antiproliferative activity against non-small cell lung cancer cell line (unknown origin) Antiproliferative activity against non-small cell lung cancer cell line (unknown origin)	[PMID: 33077264]
PANC-1	IC₅₀	701 nM Compound: Abemaciclib	Antiproliferative activity against human PANC1 cells Antiproliferative activity against human PANC1 cells	[PMID: 31200237]
PC-3	IC₅₀	9214 nM Compound: Abemaciclib	Antiproliferative activity against human PC3 cells Antiproliferative activity against human PC3 cells	[PMID: 31200237]
RPMI-8226	GI₅₀	1.479 μM Compound: Abemaciclib	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]
SF-539	EC₅₀	3.22 μM Compound: 3	Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
Sf9	IC₅₀	0.005 μM Compound: Abemaciclib	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	0.01 μM Compound: Abemaciclib	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	0.065 μM Compound: Abemaciclib	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	0.101 μM Compound: Abemaciclib	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	0.273 μM Compound: Abemaciclib	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	0.347 μM Compound: Abemaciclib	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	0.371 μM Compound: Abemaciclib	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	0.371 μM Compound: LY2835219	Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP	[PMID: 26741853]
Sf9	IC₅₀	0.405 μM Compound: Abemaciclib	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	3.1 μM Compound: Abemaciclib	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]
SiHa	IC₅₀	861 nM Compound: Abemaciclib	Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
SK-BR-3	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human SK-BR-3 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human SK-BR-3 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
SK-HEP1	IC₅₀	411 nM Compound: Abemaciclib	Antiproliferative activity against human SKHEP1 cells Antiproliferative activity against human SKHEP1 cells	[PMID: 31200237]
SNU-5	IC₅₀	523 nM Compound: Abemaciclib	Antiproliferative activity against human SNU5 cells Antiproliferative activity against human SNU5 cells	[PMID: 31200237]
T47D	GI₅₀	0.771 μM Compound: Abemaciclib	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]
T47D	IC₅₀	145 nM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
T47D	IC₅₀	34.3 nM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
T98G	EC₅₀	0.54 μM Compound: 3	Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
THP-1	IC₅₀	187 nM Compound: Abemaciclib	Antiproliferative activity against human THP1 cells Antiproliferative activity against human THP1 cells	[PMID: 31200237]
U-251	IC₅₀	294 nM Compound: Abemaciclib	Antiproliferative activity against human U251 cells Antiproliferative activity against human U251 cells	[PMID: 31200237]
U-266	GI₅₀	2.701 μM Compound: Abemaciclib	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	EC₅₀	0.12 μM Compound: 3	Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
U-87MG ATCC	IC₅₀	48.1 nM Compound: Amebaciclib	Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay	[PMID: 29247857]
U-87MG ATCC	IC₅₀	706 nM Compound: Abemaciclib	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-87MG ATCC	IC₅₀	706 nM Compound: Abemaciclib	Antiproliferative activity against human U87MG cells Antiproliferative activity against human U87MG cells	[PMID: 31200237]
Vero	CC₅₀	>50 mM Compound: 16; LY2835219	Cytotoxicity against african green monkey Vero cells Cytotoxicity against african green monkey Vero cells	[PMID: 33970631]
Vero	CC₅₀	>50 μM Compound: Abemaciclib	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	6.62 μM Compound: Abemaciclib	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
ZR-75-1	IC₅₀	83.4 nM Compound: Abemaciclib	Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]

In Vitro

Abemaciclib reduces cell viability with the IC₅₀ values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells^[1]. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC₅₀ values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC₅₀ values of 395, 260, and 463 nM, respectively^[2]. Abemaciclib inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor^[1]. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model^[2].

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

Chemical Information

CAS. Nr. 1231929-97-7
Appearance Solid
Molecular Weight 506.59
Formel C₂₇H₃₂F₂N₈
Color White to yellow
SMILES

CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C
Synonyms

LY2835219
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Publications (129)

All In Vivo Efficacy StudyWBCell Proliferation/Viability Assay

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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
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
Nature

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

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

Abemaciclib purchased from MedChemExpress. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475. [Abstract]

Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, GW572016, or Abemaciclib for 48 h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500 nM) for 0, 1, or 7 days before exposure to Staurosporine (500 nM) for 4 h.
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
Cell

A Cancer Cell Program Promotes T Cell Exclusion and Resistance to Checkpoint Blockade. [Abstract]

2018 Nov 1;175(4):984-997.e24. PMID: 30388455
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
Nat Metab

mTORC1 directly inhibits AMPK to promote cell proliferation under nutrient stress. [Abstract]

2020 Jan;2(1):41-49. PMID: 31993556
Bioact Mater

Modeling human hypertrophic scars with 3D preformed cellular aggregates bioprinting. [Abstract]

2021 Sep 8:10:247-254. PMID: 34901543
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

Bcl-xL Enforces a Slow-Cycling State Necessary for Survival in the Nutrient-Deprived Microenvironment of Pancreatic Cancer. [Abstract]

2022 May 16;82(10):1890-1908. PMID: 35315913
Cancer Res

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

2019 Oct 15;79(20):5245-5259. PMID: 31395606
Cancer Res

Kinome-Wide RNA Interference Screen Reveals a Role for PDK1 in Acquired Resistance to CDK4/6 Inhibition in ER-Positive Breast Cancer. [Abstract]

2017 May 1;77(9):2488-2499. PMID: 28249908

Abemaciclib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2017 May 1;77(9):2488-2499. [Abstract]

Treatment with PD 0332991 and Abemaciclib shows an induction of S241 P-PDK1 as early as 1 h after drug exposure without an increased in total PDK1 protein.
Cancer Res

v-Src Oncogene Induces Trop2 Proteolytic Activation via Cyclin D1. [Abstract]

2016 Nov 15;76(22):6723-6734. PMID: 27634768

Abemaciclib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Nov 15;76(22):6723-6734. [Abstract]

The effects of the CDK inhibitor Abemaciclib, PD 0332991 and Ribocilib on Trop2 ICD cleavage. CDK inhibitors decrease Trop2 ICD abundance after the 2^nd day of CDK inhibitor treatment.
Adv Funct Mater

2021 Apr 30.
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

CDK4 inactivation inhibits apoptosis via mitochondria-ER contact remodeling in triple-negative breast cancer. [Abstract]

2025 Jan 9;16(1):541. PMID: 39788939
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

Abemaciclib 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
Nat Commun

CDK4/6 and autophagy inhibitors synergistically induce senescence in Rb positive cytoplasmic cyclin E negative cancers. [Abstract]

2017 Jun 27:8:15916. PMID: 28653662
Mol Cell

Endocytosis is essential for cysteine-deprivation-induced ferroptosis. [Abstract]

2025 Sep 4;85(17):3333-3342.e4. PMID: 40858109
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
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
J Nanobiotechnology

Inhibition of METTL14 overcomes CDK4/6 inhibitor resistance driven by METTL14-m6A-E2F1-axis in ERα-positive breast cancer. [Abstract]

2025 Jan 3;23(1):3. PMID: 39754249
J Biomed Sci

CDK4/6 inhibitors synergize with radiotherapy to prime the tumor microenvironment and enhance the antitumor effect of anti-PD-L1 immunotherapy in triple-negative breast cancer. [Abstract]

2025 Aug 20;32(1):79. PMID: 40836337
J Exp Clin Cancer Res

CDK16 promotes the progression and metastasis of triple-negative breast cancer by phosphorylating PRC1. [Abstract]

2022 Apr 21;41(1):149. PMID: 35449080
Adv Sci (Weinh)

Dual Targeting of Tau Kinases and Autophagy by Abemaciclib Independent of CDK4/6 Inhibition. [Abstract]

2026 Mar;13(14):e13135. PMID: 41532696
Adv Sci (Weinh)

Two-Wave Variable Nanotheranostic Agents for Dual-Mode Imaging-Guided Photo-Induced Triple-Therapy for Cancer. [Abstract]

2022 Aug 2;e2201834. PMID: 35918610
Adv Sci (Weinh)

Charge and Size Dual Switchable Nanocage for Novel Triple-Interlocked Combination Therapy Pattern. [Abstract]

2020 Aug 4;7(18):2000906. PMID: 32999836
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
Sci Adv

LPAR4 mediates resistance to interferon-induced stress in soft tissue sarcoma. [Abstract]

2026 Jun 12;12(24):eaef1962. PMID: 42284392
Blood Cancer J

Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c). [Abstract]

2022 Jan 11;12(1):5. PMID: 35017466
Cell Death Dis

2026 Jul 1. PMID: 42380121
Cell Death Dis

Metformin as a senostatic drug enhances the anticancer efficacy of CDK4/6 inhibitor in head and neck squamous cell carcinoma. [Abstract]

2020 Oct 28;11(10):925. PMID: 33116117
Cell Death Dis

Absence of cyclin-dependent kinase inhibitor p27 or p18 increases efficiency of iPSC generation without induction of iPSC genomic instability. [Abstract]

2019 Mar 20;10(4):271. PMID: 30894510
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
Phytomedicine

Resveratrol combats Salmonella infection via liberating vacuole-enclosed bacteria for enhanced autophagic clearance and blocking HMGA2-mediated G2/M arrest. [Abstract]

2026 May:154:158042. PMID: 41812383
J Pharm Anal

Ursodeoxycholic acid inhibits the uptake of cystine through SLC7A11 and impairs de novo synthesis of glutathione. [Abstract]

2025 Jan;15(1):101068. PMID: 39902457
Clin Cancer Res

CDKN2A/B homozygous deletion sensitizes IDH-mutant glioma to CDK4/6 inhibition. [Abstract]

2024 Jul 15;30(14):2996-3005. PMID: 38718141
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086

Abemaciclib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]

MCL17-PDX mice were treated as indicated: vehicle (n = 5), abemaciclib (50 mg/kg, oral, daily; n = 5), and volasertib (5 mg/kg, intraperitoneal, weekly; n = 5). Tumor size was measured every 7 days during the treatment. Tumor volume = length x width2/2. Mice were euthanized after 21 days of treatment. Tumors were excised and weighed in comparison between each group.
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
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
Int J Biol Macromol

Molecular interaction of abemaciclib with human serum albumin: Insights from spectroscopy, microscopy, and computational approaches. [Abstract]

2025 Dec 9;337(Pt 2):149613. PMID: 41380878
Int J Mol Med

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

2025 Nov;56(5):167. PMID: 40808344
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
EMBO J

Cyclophilin D plays a critical role in the survival of senescent cells. [Abstract]

2024 Dec;43(23):5972-6000. PMID: 39448884
EMBO J

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

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

Pharmacological CDK4/6 inhibition reveals a p53-dependent senescent state with restricted toxicity. [Abstract]

2022 Mar 15;41(6):e108946. PMID: 34985783
Free Radic Biol Med

Targeted delivery of nebivolol via lactoferrin-modified liposomes inhibits NEK7-mediated pyroptosis to ameliorate inflammatory bowel disease. [Abstract]

2026 Aug 16:252:493-508. PMID: 42061481
Clin Transl Med

Oncogenic driver and therapeutic target: Prolactin signalling axis in retroperitoneal sarcoma. [Abstract]

2026 May;16(5):e70669. PMID: 42083506
EMBO Mol Med

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

2025 Aug 29. PMID: 40883610
Br J Cancer

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

2022 Jun;126(11):1616-1626. PMID: 35031765
ACS Appl Mater Interfaces

Artificial Assembled Macrophage Co-Deliver Black Phosphorus Quantum Dot and CDK4/6 Inhibitor for Colorectal Cancer Triple-Therapy. [Abstract]

2022 May 11;14(18):20628-20640. PMID: 35477252
Cell Rep

IMPDH2 dephosphorylation under FGFR signaling promotes S-phase progression and tumor growth. [Abstract]

2024 Dec 30;44(1):115116. PMID: 39739531
Cell Rep

BCL-xL inhibition potentiates cancer therapies by redirecting the outcome of p53 activation from senescence to apoptosis. [Abstract]

2022 Dec 20;41(12):111826. PMID: 36543138
Cell Rep

CDK14 inhibition reduces mammary stem cell activity and suppresses triple negative breast cancer progression. [Abstract]

2022 Sep 13;40(11):111331. PMID: 36103813
Cell Rep

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

2017 Oct 31;21(5):1386-1398. PMID: 29091774
J Med Chem

Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. [Abstract]

2023 Mar 23;66(6):4106-4130. PMID: 36876904
Sci Data

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

2024 Sep 19;11(1):1024. PMID: 39300112
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
Mol Cancer Ther

AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]

2024 Oct 1;23(10):1404-1417. PMID: 38894678
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
Acta Neuropathol Commun

Identifying and exploiting combinatorial synthetic lethality by characterizing adaptive kinome rewiring of EGFRvIII-driven glioblastoma. [Abstract]

2025 Jun 28;13(1):143. PMID: 40581663
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

Abemaciclib purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2017 Jan 15:124:29-42. [Abstract]

Effect of LY2835219 on the expression of ABCB1 or ABCG2 in MDR cells. The protein level of ABCB1 and ABCG2 on MDR cells after 0, 0.1, 0.2 and 0.4 μM LY2835219 stimulation for 48h are measured by Western blot analysis, and mRNA level are measured by PCR (GAPDH as loading control).
Cancer Gene Ther

Abemaciclib impairs glioblastoma sphere formation by targeting the GSK3β-mediated transcriptional regulation of CD44 and TCF7L2. [Abstract]

2025 Aug 14. PMID: 40813896
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
Commun Biol

A genome-scale CRISPR Cas9 dropout screen identifies synthetically lethal targets in SRC-3 inhibited cancer cells. [Abstract]

2021 Mar 25;4(1):399. PMID: 33767353
Pharmaceuticals (Basel)

Development and Application of an UPLC-MS/MS Method for Simultaneous Quantification of Abemaciclib and Tamoxifen with Their Active Metabolites in Rat Plasma: Application to a Pharmacokinetic Study. [Abstract]

2026 May 19;19(5):795. PMID: 42198468
Int J Mol Sci

Roxadustat Inhibits Osteoclast Differentiation and Function by Disrupting Cell Cycle Exit. [Abstract]

2026 Jun 18;27(12):5506. PMID: 42353219
Int J Mol Sci

Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]

2022 Feb 24;23(5):2493. PMID: 35269635
Int J Mol Sci

Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs). [Abstract]

2021 Jan 8;22(2):575. PMID: 33430060
Transl Oncol

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

2025 Feb:52:102264. PMID: 39756156
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
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

Drug-induced PD-L1 expression and cell stress response in breast cancer cells can be balanced by drug combination. [Abstract]

2019 Oct 22;9(1):15099. PMID: 31641154
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

Abemaciclib 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.
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
Biochim Biophys Acta Mol Cell Res

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

2018 Feb;1865(2):354-363. PMID: 29157894
J Biol Chem

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

2025 Feb;301(2):108196. PMID: 39826695
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
Nutrition

β-hydroxy-β-methylbutyrate (HMB) improves mitochondrial function in myocytes through pathways involving PPARβ/δ and CDK4. [Abstract]

2019 Apr:60:217-226. PMID: 30677545
Transl Lung Cancer Res

CDK4/6 inhibitor abemaciclib combined with low-dose radiotherapy enhances the anti-tumor immune response to PD-1 blockade by inflaming the tumor microenvironment in Rb-deficient small cell lung cancer. [Abstract]

2024 May 31;13(5):1032-1046. PMID: 38854937
Front Oncol

Patient-Derived Xenograft Models for Intrahepatic Cholangiocarcinoma and Their Application in Guiding Personalized Medicine. [Abstract]

2021 Jul 13:11:704042. PMID: 34327143
Biochem Biophys Rep

Efficacy of a combination therapy targeting CDK4/6 and autophagy in a mouse xenograft model of t(8;21) acute myeloid leukemia. [Abstract]

2021 Aug 13:27:101099. PMID: 34430715
J Cell Biochem

Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]

2023 Sep;124(9):1404-1422. PMID: 37566640
R Soc Open Sci

Identification of reactive intermediate formation and bioactivation pathways in Abemaciclib metabolism by LC-MS/MS: in vitro metabolic investigation. [Abstract]

2019 Jan 23;6(1):181714. PMID: 30800400
Fundam Clin Pharmacol

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

2021 Oct;35(5):919-929. PMID: 33523504
Biochem Biophys Res Commun

The CDK4/6-UCHL5-BRD4 axis confers resistance to BET inhibitors in MLL-rearranged leukemia cells by suppressing BRD4 protein degradation. [Abstract]

2022 Jan 15:588:147-153. PMID: 34954522
Biochem Biophys Res Commun

Ploidy-dependent change in cyclin D2 expression and sensitization to cdk4/6 inhibition in human somatic haploid cells. [Abstract]

2018 Sep 26;504(1):231-237. PMID: 30193733
Leuk Res

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

2022 Sep:120:106920. PMID: 35872339
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
Anticancer Res

Trametinib Synergized With Abemaciclib to Inhibit Tumor Growth in Human Head and Neck Squamous Cell Carcinoma Cells. [Abstract]

2025 Jun;45(6):2285-2295. PMID: 40425343
Biomed Chromatogr

Simultaneous quantification of abemaciclib and letrozole in rat plasma: method development, validation and pharmacokinetic application. [Abstract]

2020 Jun;34(6):e4825. PMID: 32166756
STAR Protoc

Establishment and Use of Patient-Derived Xenograft Models for Drug Testing in Head and Neck Squamous Cell Carcinoma. [Abstract]

2020 Jun 3;1(1):100024. PMID: 33111077
Gene Rep

2026 Jan 3;42:102413.
Biomed Pharmacother

2026 Sep:202:119803. PMID: 42537395
Cell Press Blue

2026 Jul 3.
bioRxiv

2026 May 25.
University of California, Los Angeles

2026.
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 Apr 19.
bioRxiv

2026 Feb 23.
bioRxiv

2026 Jan 25.
bioRxiv

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

2025 Nov 3:2025.11.02.685764. PMID: 41279360
bioRxiv

2025 Sep 15.
Biomed Pharmacother

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

2025 Aug:189:118340. PMID: 40651458
Dartmouth College

2025.
bioRxiv

Antigenic cancer persister cells survive direct T cell attack. [Abstract]

2025 Mar 17:2025.03.14.643359. PMID: 40166148
bioRxiv

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

2024 Dec 10:2024.12.09.627542. PMID: 39713309
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
SSRN

2023 Sep 29.
Heliyon

CDK4/6i enhances the antitumor effect of PD1 antibody by promoting TLS formation in ovarian cancer. [Abstract]

2023 Sep 14;9(9):e19760. PMID: 37809574
bioRxiv

A Cell Cycle-Dependent Ferroptosis Sensitivity Switch Governed by EMP2. [Abstract]

2023 Jul 19:2023.07.19.549715. PMID: 37502927
bioRxiv

2023 Jul 17.
University of Gothenburg

2023 Jun 27.
bioRxiv

2023 Jan 25.
SSRN

2022 Nov 21.
J Oncol

Trained Immunity of IL-12-, IL-15-, and IL-18-Induced CD3+CD56+ NKT-Like Cells. [Abstract]

2022 Jun 23;2022:8724933. PMID: 35783158
Department of Biochemistry

2020 Oct.
bioRxiv

2020 Jun.
Patent

US20200108066A1
J Oncol

TP53 Mutations Promote Immunogenic Activity in Breast Cancer. [Abstract]

2019 Jun 2:2019:5952836. PMID: 31275382
Oncotarget

The addition of abemaciclib to sunitinib induces regression of renal cell carcinoma xenograft tumors. [Abstract]

2017 Jul 27;8(56):95116-95134. PMID: 29221116

Abemaciclib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]

Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.

Abemaciclib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]

Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.
Oncotarget

GTSE1: a novel TEAD4-E2F1 target gene involved in cell protrusions formation in triple-negative breast cancer cell models. [Abstract]

2017 Jun 27;8(40):67422-67438. PMID: 28978043

Abemaciclib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 27;8(40):67422-67438. [Abstract]

GTSE1 protein and mRNA levels in MDA-MB-157 and MDA-MB-231 cell lines treated respectively with Abemaciclib 0.5 μM for 24h. Data are presented as mean±SEM of three independent experiments.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 2.94 mg/mL (5.80 mM; ultrasonic and warming and heat to 80°C; 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

1.9740 mL

9.8699 mL

19.7398 mL

5 mM

0.3948 mL

1.9740 mL

3.9480 mL

10 mM

---

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: 0.5% Hydroxyethyl cellulose in Water

Solubility: 3.33 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
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- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 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)

Verweise

[1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13. [Content Brief]

[2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63. [Content Brief]

[3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37. [Content Brief]

[4]. Solmaz Sahebjam et al. Assessment of concentrations of abemaciclib and its major active metabolites in plasma, CSF, and brain tumor tissue in patients with brain metastases secondary to hormone receptor positive (HR+) breast cancer. J Clin Oncol 34. 2016, 526-526.

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	1 mM	1.9740 mL	9.8699 mL	19.7398 mL	49.3496 mL
DMSO	5 mM	0.3948 mL	1.9740 mL	3.9480 mL	9.8699 mL

Bioz

Keywords

Abemaciclib

129 Cited Publications

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Abemaciclib

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