849550-67-0
849550-67-0 structure
- Name: Cevipabulin fumarate
- Chemical Name: (E)-but-2-enedioic acid,5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
- CAS Number: 849550-67-0
- Molecular Formula: C22H22ClF5N6O5
- Molecular Weight: 580.89200
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Microtubule/Tubulin
- Create Date: 2016-03-06 01:06:36
- Modify Date: 2024-01-06 19:27:10
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Cevipabulin fumarate (TTI-237 fumarate) is a microtubule-active, oral active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2].
| Name | (E)-but-2-enedioic acid,5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
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| Synonyms |
UNII-9FDJ70N1KZ
Cevipabulin fumarate anhydrous |
| Description | Cevipabulin fumarate (TTI-237 fumarate) is a microtubule-active, oral active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2]. |
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| Related Catalog | |
| Target |
IC50: 18-40 nM (microtubule in human tumor cells)[1]. |
| In Vitro | Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC50 values) on cell lines from ovarian, breast, prostate, and cervical tumors[1]. Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G1 nuclei and, at concentrations above 50 nM, it causes a strong G2-M block[1]. Cell Cytotoxicity Assay[1] Cell 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 IC50 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[1]. Animal Model: Athymic nu/nu female mice implanted s.c. in the flank with 1×107 LoVo human colon adenocarcinoma cells[1]. 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 1×106 U87-MG human glioblastoma cells[1]. 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. |
| References |
| Molecular Formula | C22H22ClF5N6O5 |
|---|---|
| Molecular Weight | 580.89200 |
| Exact Mass | 580.12600 |
| PSA | 150.97000 |
| LogP | 4.24960 |
| Storage condition | 2-8℃ |