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1610759-22-2

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1610759-22-2 Structure

1610759-22-2 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.42±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

14.53±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack 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%.
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
Spectrum DetailBack Directory
[Spectrum Detail]

CFI-402257(1610759-22-2)1HNMR
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