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CFI-402257

Chemical Structure CFI-402257

CAS No.: 1610759-22-2

CFI-402257 (CFI402257)

Catalog No.: PC-42354Not For Human Use, Lab Use Only.

A potent and selective Mps1/TTK kinase inhibitor with Ki of 0.1 nM and cellular Mps1 EC50 of 6.5 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent and selective Mps1/TTK kinase inhibitor with Ki of 0.1 nM and cellular Mps1 EC50 of 6.5 nM; exhibit effects consistent with Mps1 kinase inhibition, specifically SAC inactivation, leading to chromosome missegregation, aneuploidy, and ultimately cell death; well-tolerated in mouse models of human cancer and orally active.

Physicochemical Properties

M.Wt 498.58
Formula C28H30N6O3
CAS No. 1610759-22-2
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 1 Month
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Solubility

DMSO: 10 mM (Need Warming and Ultrasonic)

Chemical Name

Benzamide, N-cyclopropyl-4-[7-[[(cis-3-hydroxy-3-methylcyclobutyl)methyl]amino]-5-(3-pyridinyloxy)pyrazolo[1,5-a]pyrimidin-3-yl]-2-methyl-

Clinical Information

References

1. Mason JM, et al. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132.

2. Liu Y, et al. ACS Med Chem Lett. 2016 May 6;7(7):671-5.

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