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  • CFI-402257 hydrochloride
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CFI-402257 hydrochloride

CFI-402257 hydrochloride是高度选选择性,具有口服活性的TTK/Mps1抑制剂,体外对TTK 的IC50值为1.7 nM。CFI-402257 hydrochloride 具有抗癌活性。

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0-17950
CFI-402257 hydrochloride的二维码

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  • 库存: 现货
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  • 货号: ajce55566
  • CAS: 1610677-37-6
  • 别名:
  • 分子式: C28H31ClN6O3
  • 分子量: 535.04
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity[1]. IC50: 1.7 nM (TTK in vitro)[1].


CFI-402257 is highly selective to TTK. CFI-402257 is tested against a panel of human kinases at 1 μM and inhibits none of the 262 kinases tested. CFI-402257 is a potent inhibitor of cell growth[1]. CFI-402257 (200 nM, 6 h) causes a massive increase in chromosome missegregations[2].CFI-402257 (0, 50 or 100 nM) induces a dose-dependent dysregulation of the cell cycle, resulting in an increase in the frequency of cells exhibiting an aneuploid DNA content[2].CFI-402257 exhibits effects consistent with Mps1 kinase inhibition, specifically SAC inactivation, leading to chromosome missegregation, aneuploidy, and ultimately cell death[2]. Cell Cycle Analysis[2] Cell Line: HCT116 cells.


CFI-402257 given orally QD shows dose-dependent activity in mice with established tumors from xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice. CFI-402257 demonstrates antitumor activity in a platinum-resistant PDX model of high-grade serous ovarian cancer[2]. Animal Model: Xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice[2].


[1]. Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671-5. [2]. Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132.

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