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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-PHA-848125
PHA-848125

Chemical Structure : PHA-848125

CAS No.: 802539-81-7

PHA-848125 (Milciclib, PHA848125)

货号: PC-42578Not For Human Use, Lab Use Only.

Milciclib (PHA-848125) is a potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively.

规格 价格 库存 数量
5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3280 In stock
50 mg ¥5280 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

Milciclib (PHA-848125) is a potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively.
PHA-848125 also is a potent pseudokinase ULK4 binder with Ki of 4.4 uM.
PHA-848125 shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM).
PHA-848125 inhibits cell proliferation of a wide panel of tumoral cell lines with submicromolar IC50.
PHA-848125 shows significant antitumor activity in various human xenografts.

物理化学性质&存储条件

分子量 460.5746
分子式 C25H32N8O
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

1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-

参考文献

1. Brasca MG, et al. J Med Chem. 2009 Aug 27;52(16):5152-63.

2. Degrassi A, et al. Mol Cancer Ther. 2010 Mar;9(3):673-81.

3. Albanese C, et al. Mol Cancer Ther. 2010 Aug;9(8):2243-54.

4. Albanese C, et al. Br J Pharmacol. 2013 May;169(1):156-66.

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