CasNo.1231930-82-7,Abemaciclib mesylate (LY2835219),(1231930-82-7) Suppliers

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Abemaciclib mesylate LY2835219 1231930-82-7

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Biological Activity

Description

Abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.

Targets

CDK4 [1] (Cell-free assay)	CDK6 [1] (Cell-free assay)
2 nM	10 nM

In vitro

LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. [1]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human COLO205 cells	Function assay	24 h	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	26115571
human 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	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=2 nM	26115571

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-Rb(S780) / Rb / p21; p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR; pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2;	26909611 27748766
Growth inhibition assay	Cell viability;	26909611

In vivo

LY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide. [1]