5.06313
NMS-P715
InSolution, ≥98%, 5 mM in DMSO, MPS1 Inhibitor
别名:
InSolution MPS1 Inhibitor, NMS-P715, N-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution
质量水平
方案
≥98% (HPLC)
表单
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light
储存温度
−70°C
一般描述
An orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (<10 µM), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50 = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~ 1 µM), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss.
生化/生理作用
Cell permeable: yes
Primary Target
MPS1
MPS1
Reversible: yes
包装
Packaged under inert gas
外形
A 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 (Cat. No. 475949) in DMSO.
制备说明
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. If necessary, slightly warm the vial. Use only fresh DMSO for further dilutions prior to use.
其他说明
Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett.21, 4507.
Colombo, R., et al. 2011. Cancer Res.70, 10255.
Colombo, R., et al. 2011. Cancer Res.70, 10255.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
10 - Combustible liquids
WGK
WGK 1
闪点(°F)
188.6 °F - (refers to pure substance)
闪点(°C)
87 °C - (refers to pure substance)
法规信息
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