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NMS-P715

Chemical Structure : NMS-P715

CAS No.: 1202055-32-0

NMS-P715 (NMS P715;NMS-P 715)

Catalog No.: 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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10 mg $188 In stock
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50 mg $528 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 676.7311
Formula C35H39F3N8O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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]-

References

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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