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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CDDD2-94
CDDD2-94

Chemical Structure : CDDD2-94

CAS No.: 2078047-99-9

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CDDD2-94 (CDK4 inhibitor AU2-94, CDDD 2-94)

货号: PC-72637Not For Human Use, Lab Use Only.

CDDD2-94 (AU2-94) is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, >140-fold selective for CDK4 over CDK6 (Ki=279 nM).

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2 mg ￥2480 In stock
5 mg ￥3980 In stock
10 mg ￥5980 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

CDDD2-94 (AU2-94) is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, >140-fold selective for CDK4 over CDK6 (Ki=279 nM).
CDDD2-94 is ineffective against other members of the CDK family, displays high selectivity against a panel of 369 human kinases at 1uM, with exceptionally selective-CLK, DYRKs and MYLK4 were the only kinases targeted potently.
CDDD2-94 is the most selective CDK4 inhibitor identified to date.
CDDD2-94 demonstrated antiproliferative activityagainst MV4-11 and MDA-MB-453 cell lines with GI50 of 0.107 and 0.325 uM respectively.
CDDD2-94 inhibits S780-phosphorylated Rb (pRb(S780)) and decreases transcription of Rb1 and E2F-target genes in MDA-MB-453 cells.
CDDD2-94 is well tolerated and efficacious in preclinical OC xenograft model, CDDD2-94 provides better safety profile than palbociclib towards the bone marrow.

物理化学性质&存储条件

分子量 442.561
分子式 C21H27FN8S
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-(2-((5-(4-(dimethylamino)piperidin-1-yl)pyridin-2-yl)amino)-5-fluoropyrimidin-4-yl)-N,4-dimethylthiazol-2-amine

参考文献

1. Laychiluh Bantie, et al. Gynecol Oncol. 2020 Dec;159(3):827-838.

2. Solomon Tadesse, et al. Br J Pharmacol. 2018 Jun;175(12):2399-2413.

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