| Identification | Back Directory | [Name]
CFI-400945 fumarate | [CAS]
1616420-30-4 | [Synonyms]
CFI-400945 fumarate
CFI-400945 fumarate
(CFI400945
Spiro[cyclopropane-1,3'-[3H]indol]-2'(1'H)-one, 2-[3-[(1E)-2-[4-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5'-methoxy-, (1R,2S)-, (2E)-2-butenedioate (1:1) | [Molecular Formula]
C37H38N4O7 | [MOL File]
1616420-30-4.mol | [Molecular Weight]
650.73 |
| Hazard Information | Back Directory | [Uses]
CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively. | [in vivo]
Oral administration of CFI-400945 (3.0, 9.4 mg/kg) to mice bearing human cancer xenografts results in the significant inhibition of tumor growth at doses that are well tolerated. Increased antitumor activity is observed in PTEN-deficient compared to PTEN wild-type cancer xenografts. The maximum tolerated dose for once-daily administration of CFI-400945 is estimated to be 7.5-9.5 mg/kg[2]. | [IC 50]
PLK4: 2.8 nM (IC50); AURKA: 140 nM (IC50); AURKB/INCENP: 98 nM (IC50); TIE2/TEK: 22 nM (IC50); TRKA: 6 nM (IC50); TRKB: 9 nM (IC50) | [References]
[1] Sampson PB, et al. The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. J Med Chem. 2015 Jan 8;58(1):147-69. PMID:25723005
[2] Mason JM, et al. Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent. Cancer Cell. 2014 Aug 11;26(2):163-76. DOI:10.1016/j.ccr.2014.05.006 |
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| Company Name: |
ChemeGen
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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