Home Cell Cycle CDK inhibitor Abemaciclib For research use only.

Abemaciclib

Synonyms: LY2835219

Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.

Abemaciclib Chemical Structure

Abemaciclib Chemical Structure

CAS: 1231929-97-7

Selleck's Abemaciclib has been cited by 99 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Products often used together with Abemaciclib

Palbociclib (PD-0332991) HCl

Abemaciclib and Palbociclib HCl are CDK4/6 inhibitors that inhibit SARS-CoV-2 replication in AT2 and NKX2-5 cells.

Rudraraju R, et al. Stem Cell Reports. 2023 Jun 13;18(6):1308-1324.

Ribociclib

Abemaciclib and Ribociclib have been approved by the FDA for their use together with endocrine therapy such as aromatase inhibitors (AIs) or fulvestrant as therapeutic options for treatment of breast cancer.

Eggersmann TK, et al. BioDrugs. 2019 Apr;33(2):125-135.

Olaparib (AZD2281)

Ademaciclib and Olaparib combination treatment increases the percentage of sub-G1 cells to a great extent in C4–2b, C4–2b-ENZR, and NCI-H660 models.

Wu C, et al. Mol Cancer Ther. 2021 Sep;20(9):1680-1691.

Trametinib (GSK1120212)

Abemaciclib with Trametinib synergistically reduces the survival of the RAS-mutant RMS cell line RD.

Candido MF, et al. Pharmaceutics. 2023 Feb 16;15(2):664.

Paclitaxel

Abemaciclib and Paclitaxel are effective in inhibiting tumor growth compared to paclitaxel alone in cervical cancer mouse model.

Liu Y, et al. Fundam Clin Pharmacol. 2021 Feb;35(1):156-164.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COLO205 cells Function assay 24 h 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, IC50=0.12 μM 26115571
SK-ES-1 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
Cado-ES-1 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-7 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
TC-71 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
A673 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
RD-ES Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-1 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-3 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
CHLA-258 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
MHH-ES-1 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-8 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
EW8 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-6 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-2 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
SMS-CTR Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
ES-4 Proliferation assay 96 hours antiproliferative effects with an absolute EC50 value below 1 μmol/L 30131386
CT26 Cell viability assay 96 hours IC50=2.7 μM 29539425
insect cells Function assay 50 mins Competitive inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP, Ki = 0.0006 μM. 26115571
insect cells Function assay 50 mins Inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by microplate scintillation counter, IC50 = 0.002 μM. 26115571
COLO205 Function assay 24 hrs Inhibition of CDK4/6 in human COLO205 cells assessed as maximum cell cycle arrest at G1 phase after 24 hrs by propidium iodide staining-based flow cytometric analysis, INH = 6.7 μM. 26115571
Sf9 Function assay 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, IC50 = 0.371 μM. 26741853
Sf9 Function assay 90 mins Inhibition of recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation countin, Ki = 0.002 μM. 27171036
Sf9 Function assay 90 mins Inhibition of recombinant full length human N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintilla, Ki = 0.01 μM. 27171036
Sf21 Function assay Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide, Ki = 3.91 μM. 27171036
COLO205 Antiproliferative assay 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay, IC50 = 0.46 μM. 29074254
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay, IC50 = 0.0481 μM. 29247857
Sf9 Function assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method, IC50 = 0.002 μM. 29429832
Sf9 Function assay 90 mins Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay, IC50 = 0.0078 μM. 29429832
Sf9 Function assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (M1 to A326 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method, IC50 = 0.01 μM. 29429832
Sf9 Function assay 90 mins Inhibition of recombinant human full length CDK1/Cyclin D3 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay, IC50 = 0.056 μM. 29429832
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay, IC50 = 0.191 μM. 29429832
COLO205 Antiproliferative assay 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay, IC50 = 0.217 μM. 29459274
MDA-MB-468 Antiproliferative assay 96 hrs Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay, IC50 = 4.808 μM. 29459274
COLO205 Function assay 0.1 to 10 uM 24 hrs Inhibition of CDK4 in human COLO205 cells assessed as reduction in total Rb protein level at 0.1 to 10 uM after 24 hrs by immunoblotting method 29459274
COLO205 Cell cycle arrest assay up to 10 uM 24 hrs Cell cycle arrest in human COLO205 cells assessed as accumulation at G2/M phase up to 10 uM after 24 hrs by propidium iodide staining based FACS analysis 29459274
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Biological Activity

Description Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Targets
CDK4 [1]
(Cell-free assay)		 CDK6 [1]
(Cell-free assay)
2 nM 10 nM
In vitro
In vitro Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. Besides the cell-cycle dependent activity, abemaciclib is able to boost antitumor immunity by potentiating tumor antigen presentation and selectively suppressing proliferation of regulatory T (Treg) cells at the same time[1]. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines[2]. In vitro, treatment with abemaciclib resulted in increased activation of human T cells and upregulated expression of antigen presentation genes in MCF-7 breast cancer cells[3].
Cell Research Cell lines CT26 tumor cell line
Concentrations 0-10 μM
Incubation Time 96 h
Method

Tumor cells were cultured for 4 hr alone at 37°C, and then abemaciclib, palbociclib, or DMSO control was added at indicated concentrations for 96 hr at 37°C. Cell viability was then assessed.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Rb / Rb / p-EGFR / EGFR / p-HER2 / HER2 / p-HER3 / HER3 / p-P70S6K / P70S6K / p-S6RP / S6RP / Cyclin D1 β-catenin GSK3β / CAMKII pan CDK6 / CDK4 / AXL 26977878
In Vivo
In vivo In a colorectal cancer xenograft model used to develop an integrated pharmacokinetic/pharmacodynamic model, abemaciclib can be dosed orally on a continuous schedule to achieve sustained target inhibition and demonstrates not only durable cell-cycle inhibition but also single-agent antitumor activity. Tumor growth inhibition is observed in multiple other human cancer xenograft models, including those derived from non-small cell lung cancer (NSCLC), melanoma, glioblastoma, and mantle cell lymphoma. Abemaciclib distributes across the blood–brain barrier and prolongs survival in an intracranial glioblastoma xenograft model. In human, The pharmacokinetics of abemaciclib shows a slow absorption phase with a median time from oral dose to maximum plasma concentration (tmax) ranging from 4 to 6 hours. It is extensively cleared and distributed. The mean terminal elimination half-life (t1/2) ranged from 17.4 to 38.1 hours with no apparent dose-dependent change in clearance[2].
Animal Research Animal Models Athymic nude mice implanted with human NSCLC xenograft tumors
Dosages 25, 50, or 100 mg/kg/d
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06139107 Not yet recruiting Breast Cancer Mridula George MD|Rutgers The State University of New Jersey December 21 2023 Phase 1
NCT06169371 Recruiting Breast Cancer University of Illinois at Chicago December 2023 Phase 4

Chemical lnformation & Solubility

Molecular Weight 506.59 Formula

C27H32F2N8
CAS No. 1231929-97-7 SDF --
Smiles CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 8 mg/mL

DMSO : 6 mg/mL ( (11.84 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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