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5-氯-6-[2,6-二氟-4-[3-(甲基氨基)丙氧基]苯基]-N-((1S)-2,2,2-三氟-1-甲基乙基)-[1,2,4]三唑并[1,5-A]嘧啶-7-胺

更新时间:2025-09-01 06:36:45 采购访问:30次

常用名 西维布林 CAS号 849550-05-6
价格 纯度 99.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
Cevipabulin(TTI-237) is a novel, potent, synthetic small molecule, inhibits binding of vinblastine at the Vinca alkaloid site of the αβ-tubulin heterodimer.IC50 value: Target: Antimicrotubule agentin vitro: TTI-237 inhibited the binding of [(3)H]vinblastine to tubulin, but it caused a marked increase in turbidity development that more closely resembled the effect observed with docetaxel than that observed with vincristine. When applied to cultured human tumor cells at concentrations near its IC(50) value for cytotoxicity (34 nmol/L), TTI-237 induced multiple spindle poles and multinuclear cells, as did paclitaxel, but not vincristine or colchicine. Flow cytometry experiments revealed that, at low concentrations (20-40 nmol/L), TTI-237 produced sub-G(1) nuclei and, at concentrations above 50 nmol/L, it caused a strong G(2)-M block. The compound was a weak substrate of multidrug resistance 1 (multidrug resistance transporter or P-glycoprotein). In a cell line expressing a high level of P-glycoprotein, the IC(50) of TTI-237 increased 25-fold whereas those of paclitaxel and vincristine increased 806-fold and 925-fold, respectively. TTI-237 was not recognized by the MRP or MXR transporters [1]. TTI-237 inhibited the exchange of [(3)H]GTP at the exchangeable nucleotide site of the tubulin heterodimer, and was similar to vincristine in its effects on the phosphorylation of eight intracellular proteins in HeLa cells [3].in vivo: TTI-237 was active in vivo in several nude mouse xenograft models of human cancer, including LoVo human colon carcinoma and U87-MG human glioblastoma, when dosed i.v. or p.o [1].
物理化学性质:
CAS号:849550-05-6
常用中文名:西维布林
常用英文名:Cevipabulin
分子式:C18H18ClF5N6O
分子量:464.820
密度:1.5±0.1 g/cm3
沸点:N/A
熔点:N/A
闪点:N/A
储存条件:2-8℃

供应商信息

上海化源世纪贸易有限公司 认证供应商

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参考价格:$185/10mM*1mLinDMSO
其他供应商价格:
2025-02-05 Cevipabulin
价格:¥2880.9
2023-09-15 Cevipabulin
价格:¥需询单
2021-02-06 Cevipabulin
价格:¥2989.0

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