Chemical Structure : CCT-251455
货号: PC-61144Not For Human Use, Lab Use Only.
CCT-251455 is a potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).
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CCT-251455 is a potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).
CCT-251455 stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding.
CCT-251455 inhibits HCT116 cell growth with GI50 of 0.16 uM, dose-dependently inhibits MPS1 in HCT116 human tumor xenograft model.
分子量 | 503.991 | |
分子式 | C26H26ClN7O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Naud S, et al. J Med Chem. 2013 Dec 27;56(24):10045-65.
2. Gurden MD, et al. Cancer Res. 2015 Aug 15;75(16):3340-54.
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