Cevipabulin fumarate(Synonyms: TTI-237 fumarate)

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Cevipabulin fumarate (Synonyms: TTI-237 fumarate) 纯度: 99.08%

Cevipabulin fumarate (TTI-237 fumarate) 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 fumarate(Synonyms: TTI-237 fumarate)

Cevipabulin fumarate Chemical Structure

CAS No. : 849550-67-0

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10 mM * 1 mL in DMSO ￥2147 In-stock
5 mg ￥1680 In-stock
10 mg ￥2880 In-stock
50 mg ￥8880 In-stock
100 mg ￥12400 In-stock
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生物活性

Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2].

IC50 & Target

IC50: 18-40 nM (microtubule in human tumor cells)[1].
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 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 1×107 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.

Clinical Trial

分子量

580.89

Formula

C22H22ClF5N6O5
CAS 号

849550-67-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (86.07 mM; Need ultrasonic)

H2O : 1.43 mg/mL (2.46 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7215 mL 8.6075 mL 17.2150 mL
5 mM 0.3443 mL 1.7215 mL 3.4430 mL
10 mM 0.1721 mL 0.8607 mL 1.7215 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Beyer CF, et al. TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer Res. 2008 Apr 1;68(7):2292-300.

    [2]. Beyer CF, et al. The microtubule-active antitumor compound TTI-237 has both DB01229-like and Leurocristine-like properties. Cancer Chemother Pharmacol. 2009 Sep;64(4):681-9.

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