Abemaciclib (Synonyms: LY2835219)

目录号: HY-16297A 纯度: 99.97%: Data Sheet SDS COA 产品使用指南
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Abemaciclib (LY2835219) 是具有选择性的 CDK4/6 抑制剂，能够抑制 CDK4/CDK6 的活性，IC₅₀ 分别为 2 nM 和 10 nM。

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Abemaciclib Chemical Structure

CAS No. : 1231929-97-7

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Other Forms of Abemaciclib:

MCE 顾客使用本产品发表的 105 篇科研文献

: Abemaciclib purchased from MCE. 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.

: Abemaciclib purchased from MCE. 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.

: Abemaciclib purchased from MCE. 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).

: Abemaciclib purchased from MCE. 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.

: Abemaciclib purchased from MCE. 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 MCE. 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.

: Abemaciclib purchased from MCE. 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.

: Abemaciclib purchased from MCE. 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.

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Abemaciclib (LY2835219) is a selective 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)

细胞效力
(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]
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]
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]
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]
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]
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]
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	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-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-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	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]
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]
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]
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]
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]
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 U87MG cells Antiproliferative activity against human U87MG cells	[PMID: 31200237]
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]
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]

体外研究
(In Vitro)

Abemaciclib 可降低细胞活力，IC₅₀ 值范围为 0.5 μM 至 0.7 μM，可抑制头颈部鳞状细胞癌 (HNSCC) 细胞中的 Akt 和 ERK 信号传导，但不抑制 mTOR 活化^[1]。
Abemaciclib 对 A375R1-4、M14R 和 SH4R 有抑制作用，EC₅₀ 值范围为 0.3 至 0.6 μM；Abemaciclib 可抑制亲本 A375 和耐药 A375RV1 和 A375RV2 细胞的增殖，IC₅₀ 值分别为 395、260 和 463 nM，效果相似^[2]。
Abemaciclib 以低纳摩尔效力抑制 CDK4 和 CDK6，抑制 Rb 磷酸化，导致 G1 停滞和增殖抑制，其活性特定于 Rb 熟练的细胞^[3]。

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

体内研究
(In Vivo)

Abemaciclib（45 mg/kg，口服）与 RAD001 联合使用，在 HNSCC 异种移植肿瘤中产生协同抗肿瘤作用^[1]。
Abemaciclib（45 或 90 mg/kg，口服）在 A375 异种移植模型中表现出显著的肿瘤生长抑制作用^[2]。

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

Clinical Trial

分子量

506.59

Formula

C₂₇H₃₂F₂N₈

CAS 号

1231929-97-7

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 2.94 mg/mL (5.80 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9740 mL	9.8699 mL	19.7398 mL
5 mM	0.3948 mL	1.9740 mL	3.9480 mL
10 mM	---	---	---

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% Hydroxyethyl cellulose in Water
Solubility: 3.33 mg/mL (6.57 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.97%

选择批次：

Data Sheet (634 KB) SDS (419 KB)

COA (282 KB) HNMR (232 KB) RP-HPLC (245 KB) MS (211 KB) 元素分析报告 (205 KB)

产品使用指南 (1538 KB)

参考文献

[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]

Cell Assay ^[1]	Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between Abemaciclib and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×10⁶) cells. When tumor sizes reach approximately 100 mm³, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L×W²)/2. Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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]

Abemaciclib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Abemaciclib1231929-97-7LY2835219LY 2835219LY-2835219CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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Abemaciclib (Synonyms: LY2835219)

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Abemaciclib (Synonyms: LY2835219)

Customer Review

Other Forms of Abemaciclib:

Abemaciclib 相关抗体

MCE 顾客使用本产品发表的 105 篇科研文献

Abemaciclib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

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生物活性

实验参考方法

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参考文献

Abemaciclib 相关抗体:

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