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Abemaciclib | Potent and selective CDK 4/6 inhibitor

Abemaciclib (1231930-82-7) is a potent and selective CDK4/6 inhibitor (IC50 = 2 nM and 10 nM respectively).1 It caused G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells, and MV4-11 AML cells. Abemaciclib was also active in several human tumor xenograft models. It displayed 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.2 Abemaciclib induced a T cell inflamed tumor microenvironment and enhanced the efficacy of PD-L1 checkpoint blockade in MCF-7 breast cancer cells.3 FDA approved for the treatment of advanced breast cancers.

References/Citations
1) Gelbert et al. (2014), Preclinical characterization of the CDK4/6 inhibitor LY2835219: In-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine; Invest. New Drugs, 32 825
2) Patnail et al. (2016), Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-small Cell Lung Cancer, and Other Solid Tumors; Cancer Discov., 6 740
3) Schaer et al. (2018), The CDK4/6 Inhibitor Abemaciclib Induces a T Cell Inflamed Tumor Microenvironment and Enhances the Efficacy of PD-L1 Checkpoint Blockade; Cell Rep., 22 2978

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Catalog#  10-4833-0005

$50.00
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CAS:
1231930-82-7
Catalog Number:
10-4833
Activity:
Potent and selective CDK 4/6 inhibitor
Chemical 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 Name:
LY2835219 mesylate
Molecular Weight:
602.70
Molecular Formula:
C27H32F2N8 ∙ CH3SO3H
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to at least 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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