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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CDKI-73
CDKI-73

Chemical Structure : CDKI-73

CAS No.: 1421693-22-2

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CDKI-73 (Asnuciclib, CDKI73, LS-007)

货号: PC-43037Not For Human Use, Lab Use Only.

Asnuciclib (CDKI-73) is a potent CDK9 inhibitor with Ki of 4 nM, shows cytotoxicity against a broad CLL samples with mean LD50 of 80 nM.

规格 价格 库存 数量
2 mg ￥1580 In stock
5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Asnuciclib (CDKI-73) is a potent CDK9 inhibitor with Ki of 4 nM, shows cytotoxicity against a broad CLL samples with mean LD50 of 80 nM.
CDKI-73 induces caspase-dependent apoptosis that was preceded by dephosphorylation of CDK9 and serine 2 of RNA polymerase II.
CDKI-73 is more potent than the pan-CDK inhibitor Flavopiridol and shows >200-fold selectivity against primary leukemia cells when compared with normal CD34+ cells.
CDKI-73 shows cytotoxic synergy with the nucleoside analog fludarabine in in poor prognostic sub-groups of leukemia patients, which is associated with CDKI-73-mediated transcriptional inhibition of MCL1 and XIAP.

物理化学性质&存储条件

分子量 394.447
分子式 C15H15FN6O2S2
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

Benzenesulfonamide, 3-[[5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-pyrimidinyl]amino]-

参考文献

1. Walsby E, et al. Oncotarget. 2014 Jan 30;5(2):375-85.

2. Lam F, et al. Oncotarget. 2014 Sep 15;5(17):7691-704.

3. Cao S, et al. Biochem Biophys Res Commun. 2017 Jan 22;482(4):536-541.

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