| Identification | Back Directory | [Name]
CFI-402257 | [CAS]
1610759-22-2 | [Synonyms]
CS-2627
CFI-402257
luvixasertib
CFI402257;CFI 402257;CFI-402257
Benzamide, N-cyclopropyl-4-[7-[[(cis-3-hydroxy-3-methylcyclobutyl)methyl]amino]-5-(3-pyridinyloxy)pyrazolo[1,5-a]pyrimidin-3-yl]-2-methyl- | [Molecular Formula]
C28H30N6O3 | [MDL Number]
MFCD31382135 | [MOL File]
1610759-22-2.mol | [Molecular Weight]
498.58 |
| Hazard Information | Back Directory | [Uses]
CFI-402257 is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 has anti-cancer activity[1]. | [in vivo]
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]. | | Dosage: | 5, 6 mg/kg. | | Administration: | Oral gavage, daily. | | Result: | Xenografted MDA-MB-231 human TNBC cells: 5 mg/kg, tumor growth inhibition (TGI) = 74%; 6 mg/kg, TGI = 89%.
Xenografted MDA-MB-468 human TNBC cells: 5 mg/kg, tumor growth inhibition (TGI) = 75%; 6 mg/kg, TGI = 94%.
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| Animal Model: | PDX model of high-grade serous ovarian cancer[2]. | | Dosage: | 6.5, 7.5 mg/kg. | | Administration: | Oral gavage, daily. | | Result: | 6.5 mg/kg, tumor growth inhibition (TGI) = 61%; 7.5 mg/kg, TGI = 97%.
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| [References]
[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. DOI:10.1021/acsmedchemlett.5b00485
[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. DOI:10.1073/pnas.1700234114 |
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| Company Name: |
Cckinase, Inc.
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| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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