Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [ 3 H]NSC 49842 to tubulin, with an IC 50 of 18-40 nM for cytotoxicity in human tumor cell line In Vitro Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC 50 values) on cell lines from ovarian, breast, prostate, and cervical tumors. Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G 1 nuclei and, at concentrations above 50 nM, it causes a strong G 2 -M block. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: Human cancer cell lines (SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP, and Hela cells). Concentration: 0-50 nM Incubation Time: 72 hours Result: The IC 50 values are 24±8 nM, 21±4 nM, 18±6 nM, 22±7 nM and 40 nM in SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP and Hela cells. In Vivo Cevipabulin (TTI-2370)( 5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles, in mice) is active by i.v. and p.o. administration against human tumor xenografts, showing dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic nu/nu female mice implanted s.c. in the flank with 1×10 7 LoVo human colon adenocarcinoma cells . Dosage: 5, 10, 15, and 20 mg/kg Administration: I.V. injection every 4 days for 4 cycles. Result: The compound showed dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg. Animal Model: Athymic nu/nu female mice implanted s.c. in the flank with 1×10 6 U87-MG human glioblastoma cells . Dosage: 25 mg/kg. Administration: P.O. or I.V. on days 0, 7, 14. Result: The compound was active by p.o. or i.v. administration against human tumor xenografts. Form:Solid IC50& Target:IC50: 18-40 nM (microtubule in human tumor cells)
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Cevipabulin fumarate
CAS number：849550-67-0 molecular formula：C22H22ClF5N6O5
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| Chinese alias | 富马酸西维帕布林 | ||
| English alias | Cevipabulin fumarate | Cevipabulin fumarate anhydrous | UNII-9FDJ70N1KZ | 5-CHLORO-6-(2,6-DIFLUORO-4-(3-(METHYLAMINO)PROPOXY)PHENYL)-N-((1S)-2,2,2-TRIFLUORO-1-METHYLETHYL)-(1,2,4)TRIAZOLO(1,5-A)PYRIMIDIN-7-AMINE (2E)-BUT-2-ENEDIOATE (1:1) | 5-Chloro-6-[2, | ||
| CAS number | 849550-67-0 | molecular formula | C22H22ClF5N6O5 |
| molecular weight | 580.89 g/mol | Exact mass | ≥99% |
| PSA | 151.000 Ų | logp | - |
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