CFI-402257
- Product Name
- CFI-402257
- CAS No.
- 1610759-22-2
- Chemical Name
- CFI-402257
- Synonyms
- CS-2627;CFI-402257;luvixasertib;CFI402257,CFI 402257;Luvixasertib (CFI-402257);CFI402257;CFI 402257;CFI-402257;N-Cyclopropyl-4-(7-(((cis-3-hydroxy-3-methylcyclobutyl)methyl)amino)-5-(pyridin-3-yloxy)pyrazolo[1,5-a]pyrimidin-3-yl)-2-methylbenzamide;Benzamide, N-cyclopropyl-4-[7-[[(cis-3-hydroxy-3-methylcyclobutyl)methyl]amino]-5-(3-pyridinyloxy)pyrazolo[1,5-a]pyrimidin-3-yl]-2-methyl-
- CBNumber
- CB33175531
- Molecular Formula
- C28H30N6O3
- Formula Weight
- 498.58
- MOL File
- 1610759-22-2.mol
CFI-402257 Property
- Density
- 1.42±0.1 g/cm3(Predicted)
- pka
- 14.53±0.20(Predicted)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 21960
- Product name
- CFI-402257
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $98
- Updated
- 2021/12/16
- Product number
- 21960
- Product name
- CFI-402257
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $441
- Updated
- 2021/12/16
CFI-402257 Chemical Properties,Usage,Production
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%. |
| 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%. |
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
CFI-402257 Preparation Products And Raw materials
Raw materials
Preparation Products
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