Abemaciclib, CDK 4/6 inhibitor (TBI4833)

Description

Product Details

Formal Name: N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridine-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine methanesulfonic acid salt

Alternate Names: LY2835219 mesylate

Molecular Formula: C₂₇H₃₂F₂N₈·CH₃SO₃H

Formula Weight: 602.70

CAS Number: 1231930-82-7

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

CDK 4/6 inhibitor

Functions

Potent and selective CDK4/6 inhibitor (IC50 = 2 nM and 10 nM respectively). Induces G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells, and MV4-11 AML cells; also active in several human tumor xenograft models. Displays efficacy in patients with various solid tumors including breast cancer, non-small cell lung cancer, glioblastoma, melanoma, colorectal cancer, and hormone receptor-positive breast cancer. Abemaciclib induced a T cell inflamed tumor microenvironment and enhanced the efficacy of PD-L1 checkpoint blockade in MCF-7 breast cancer cells. FDA approved for the treatment of advanced breast cancers.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml) or in Water (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.