| Identification | Back Directory | [Name]
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 | [CAS]
849550-05-6 | [Synonyms]
TTI237
CS-1680
D06576.
TTI 237
Cevipabulin
TTI237; D06576
Unii-p14m0dws2j
Cevipabulin (TTI-237)
Cevipabulin (free base)
TTI 237; TTI237; TTI237; D06576.
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
[1,2,4]Triazolo[1,5-a]pyrimidin-7-amine, 5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-N-[(1S)-2,2,2-trifluoro-1-methylethyl]- | [Molecular Formula]
C18H18ClF5N6O | [MDL Number]
MFCD09832720 | [MOL File]
849550-05-6.mol | [Molecular Weight]
464.82 |
| Hazard Information | Back Directory | [Uses]
Cevipabulin (TTI-237) is an oral, microtubule-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]. | [Biological Activity]
cevipabulin (tti-237) is a new anti-microtubule agent [1][2][3][4].microtubules are a component of the cytoskeleton that participate in many crucial cellular functions, include maintaining the structure of the cell, forming the cytoskeleton and chromosome separation.cevipabulin (tti-237) is a new anti-microtubule agent with antitumor activity. in colo 205 cells, tti-237 inhibited cell proliferation with ic50 value of 31 nm [1]. at low ratios of tti-237: tubulin heterodimer (about 1:30), tti-237 increased depolymerization kinetics in response to low temperature, but stabilized the aggregates at high ratios (about 1:4). tti-237 inhibited the exchange of [3h]gtp at the exchangeable nucleotide site of the tubulin heterodimer [2]. cevipabulin (tti-237) increased tubulin polymerization. cevipabulin was stable and water-soluble, and could be administered i.v. or p.o. in saline [3]. tti-237 inhibited the binding of [3h]vinblastine to tubulin, but significantly increased turbidity development that more closely resembled the effect of docetaxel. in hela cells, tti-237 (34 nmol/l) induced multiple spindle poles and multi-nuclear cells. at 20-40 nmol/l, tti-237 produced sub-g1 nuclei, while at > 50 nmol/l, tti-237 induced g2-m block.in athymic mice bearing lovo human colon adenocarcinoma, tti-237 exhibited good antitumor activity in a dose-dependent way. in mice bearing u87-mg human glioblastoma, tti-237 (25 mg/kg) given both i.v. and p.o. were equally effective [4]. | [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. | | Result: | The compound was active by p.o. or i.v. administration against human tumor xenografts. |
| [storage]
Store at -20°C | [References]
[1]. zhang n, ayral-kaloustian s, nguyen t, et al. 2-cyanoaminopyrimidines as a class of antitumor agents that promote tubulin polymerization. bioorg med chem lett, 2007, 17(11): 3003-3005.
[2]. beyer cf, zhang n, hernandez r, et al. the microtubule-active antitumor compound tti-237 has both paclitaxel-like and vincristine-like properties. cancer chemother pharmacol, 2009, 64(4): 681-689.
[3]. ayral-kaloustian s, zhang n, beyer c. cevipabulin (tti-237): preclinical and clinical results for a novel antimicrotubule agent. methods find exp clin pharmacol, 2009, 31(7): 443-447.
[4]. beyer cf, zhang n, hernandez r, et al. tti-237: a novel microtubule-active compound with in vivo antitumor activity. cancer res, 2008, 68(7): 2292-2300. |
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