Cevipabulin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cevipabulin (TTI-237) 是一种微管活性的、口服有效的抗肿瘤化合物，可抑制 [3H] 长春碱与微管蛋白的结合，对人癌细胞的 IC50 值为 18-40 nM。

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.

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.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.Cell Cytotoxicity Assay 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.

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.Animal Model:Athymic nu/nu female mice implanted s.c. in the flank with 1×107 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 1×106 U87-MG human glioblastoma cells.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.

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Others

Other Targets

Microtubule Associated

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849550-05-6

464.82

C18H18ClF5N6O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 16.67 mg/mL (35.86 mM; 超声助溶 )

[H][C@@](C)(Nc1c(c(Cl)nc2ncnn12)-c1c(F)cc(OCCCNC)cc1F)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years