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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Monopolar Spindle 1 (Mps1/TTK)-NMS-P715
NMS-P715

Chemical Structure : NMS-P715

CAS No.: 1202055-32-0

NMS-P715 (NMS P715, NMS-P 715)

货号: PC-43014Not For Human Use, Lab Use Only.

NMS-P715 is a potent, selective, orally bioavailable Mps1 inhibitor with IC50 of 8 nM, Ki of 0.99 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NMS-P715 is a potent, selective, orally bioavailable Mps1 inhibitor with IC50 of 8 nM, Ki of 0.99 nM.
NMS-P715 displays excellent selectivity in vitro against a panel of 60 kinases at 5 uM.
NMS-P715 selectively reduces cancer cell proliferation, leaving normal cells almost unaffected, promotes massive spindle assembly checkpoint (SAC) in U2OS cells with EC50 of 68 nM.
NMS-P715 causes a reduction in G1 phase and a flattening in G2/M phase of the cell cycle accompanied by histone H3 dephosphorylation, PARP cleavage, and histone H2AX phosphorylation.
NMS-P715 inhibits tumor growth in preclinical cancer models.

物理化学性质&存储条件

分子量 676.7311
分子式 C35H39F3N8O3
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

DMSO: < 6.9 mg/mL

Chemical Name/SMILES

1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, N-(2,6-diethylphenyl)-4,5-dihydro-1-methyl-8-[[4-[[(1-methyl-4-piperidinyl)amino]carbonyl]-2-(trifluoromethoxy)phenyl]amino]-

参考文献

1. Colombo R, et al. Cancer Res. 2010 Dec 15;70(24):10255-64.

2. Slee RB, et al. Mol Cancer Ther. 2014 Feb;13(2):307-315.

3. Maachani UB, et al. Mol Cancer Res. 2015 May;13(5):852-62.

4. Gurden MD, et al. Cancer Res. 2015 Aug 15;75(16):3340-54.

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