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

Chemical Structure : Bireociclib

CAS No.: 1800506-48-2

Bireociclib (XZP-3287, XZP3287)

货号: PC-24657Not For Human Use, Lab Use Only.

Bireociclib (XZP-3287) is a novel potent, selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor with IC50 of 2.7/16 nM respectively.

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5 mg ¥1980 In stock
10 mg ¥2980 In stock
25 mg ¥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Bireociclib (XZP-3287) is a novel potent, selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor with IC50 of 2.7/16 nM respectively.
Bireociclib (XZP-3287) exhibits a significantly stronger selective inhibitory effect on CDK4 than on CDK6, but with additional inhibitory activity against CDK2 and CDK9.
Bireociclib (XZP-3287) reduced the phosphorylation level of the Rb protein at Ser780, thereby impeding tumor cell division and inducing cell cycle arrest at the G0/G1 phase.
Bireociclib (XZP-3287) resulted in significant tumor regression in a ZR-75-1-R tamoxifen-resistant breast cancer model.

物理化学性质&存储条件

分子量 506.61
分子式 C27H32F2N8
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

5-((4-ethylpiperazin-1-yl)methyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyridin-2-yl)pyrimidin-2-amine

参考文献

1. Wang J, et al. Nat Commun. 2025 Apr 9;16(1):3350.

2. Patent US20180000819A1.

3. Liang B, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2025 May 16;1261:124658.

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