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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-AZD8421
AZD8421

Chemical Structure : AZD8421

CAS No.:

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AZD8421 (AZD-8421)

货号: PC-22118Not For Human Use, Lab Use Only.

AZD8421 (AZD-8421) is a potent, highly selective CDK2 inhibitor with IC50 of 9 nM, >300-fold selectivity over CDK9.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AZD8421 (AZD-8421) is a potent, highly selective CDK2 inhibitor with IC50 of 9 nM, >300-fold selectivity over CDK9.
AZD8421 forms hydrogen bonding interaction with Lys89 (a CDK2-specific residue) near the solvent region of the ATP-binding pocket.
AZD8421 displays high selectivity over CDK1, CDK4 and CDK6.
AZD8421 potently inhibits cell proliferation (69 nM, OVCAR3), correlated with inhibition of pRB, arrest in G1/S phase of the cell cycle and induction of senescence, in a CCNE1 amplified cell line.
AZD8421 shows combination benefit when combined with approved CDK4/6 inhibitors in CDK4/6 inhibitor resistant breast cancer cell lines.
AZD8421 potently suppresses phosphorylation of Rb, and demonstrates robust monotherapy and CDK4/6i combination activity in breast and ovarian in vivo models.
AZD8421 shows robust monotherapy activity in a CCNE1 amplified ovarian model OVCAR3 with regressions seen with monotherapy and in combination with palbociclib in CDK4/6 inhibitor resistant breast PDXs.

物理化学性质&存储条件

分子量 440.57
分子式 C18H32N8O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-ethyl-3-((9-ethyl-2-(((2R,3S)-2-hydroxypentan-3-yl)amino)-9H-purin-6-yl)amino)pyrrolidine-1-sulfonamide

参考文献

1. Christopher R. Denz, et al. Cancer Res (2024) 84 (7_Supplement): ND06.

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