For research use only.
Catalog No.S5716 Synonyms: LY2835219
CAS No. 1231929-97-7
Abemaciclib (LY2835219) is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Selleck's Abemaciclib has been cited by 24 publications
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Choose Selective CDK Inhibitors
|Description||Abemaciclib (LY2835219) is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.|
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. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines. 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.
|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.|
|In vitro||DMSO||6 mg/mL (11.84 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04408924||Not yet recruiting||Drug: Abemaciclib||Metastatic Castration-Resistant Prostate Cancer||Eli Lilly and Company||November 20 2020||Phase 2|
|NCT04238819||Not yet recruiting||Drug: Abemaciclib|Drug: Irinotecan|Drug: Temozolomide||Relapsed Solid Tumor|Refractory Solid Tumor||Eli Lilly and Company||October 20 2020||Phase 1|
|NCT04169074||Not yet recruiting||Drug: Abemaciclib|Drug: Abemaciclib plus nivolumab||HNSCC||University of Arizona||September 1 2020||Phase 2|
|NCT04514159||Not yet recruiting||Drug: ZN-c5|Drug: Abemaciclib||Breast Cancer||Zeno Alpha Inc.||September 2020||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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