Fosbretabulin disodium(Synonyms: CA 4DP; CA 4P; Combretastatin A4 disodium phosphate)

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Fosbretabulin disodium (Synonyms: CA 4DP; CA 4P; Combretastatin A4 disodium phosphate) 纯度: 99.47%

Fosbretabulin disodium (CA 4DP) 是微管蛋白去稳定剂。Fosbretabulin disodium 是 Combretastatin A4 前药，可选择性靶向内皮细胞，诱导新生肿瘤新血管消退，减少肿瘤血流量并引起中央肿瘤坏死。

Fosbretabulin disodium(Synonyms: CA 4DP; CA 4P; Combretastatin A4 disodium phosphate)

Fosbretabulin disodium Chemical Structure

CAS No. : 168555-66-6

规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥982 In-stock
5 mg ￥893 In-stock
10 mg ￥1200 In-stock
50 mg ￥3500 In-stock
100 mg ￥6000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 prodrug that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis[1][3].

IC50 & Target

tubulin[1]
体外研究
(In Vitro)

Fosbretabulin disodium inhibits growth of leukemia P-388, pancreas BXPC-3, neuroblast SK-N-SH, thyroid SW1736, lung-NSC NCI-H460, prostate DU-145, an pharynx FADU, with EC50s of 0.0029, 0.23, 0.00025, 0.00061, 0.00035, 0.00072, and 0.00045 μg/mL, respectively[2].

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.
体内研究
(In Vivo)

Fosbretabulin disodium (100 mg/kg; i.p.) increases the mean arterial blood pressure (MABP) at 1 and 6 h after administration and decreases the tumor blood flow in rats[3].

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: Male BD9 rats (7-9 weeks) bearing the s.c. implanted P22 tumor[3]
Dosage: 100 mg/kg
Administration: A single i.p. injections
Result: Significantly raised the MABP by about 30%, and reduced the heart rate at 1 h after administration.
Reduced the blood flow in the tumor.

Clinical Trial

分子量

440.29

Formula

C18H19Na2O8P
CAS 号

168555-66-6
中文名称

康普瑞汀磷酸二钠
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: 

H2O : 4.5 mg/mL (10.22 mM; Need ultrasonic and warming)

DMF : 1 mg/mL (2.27 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2712 mL 11.3562 mL 22.7123 mL
5 mM 0.4542 mL 2.2712 mL 4.5425 mL
10 mM 0.2271 mL 1.1356 mL 2.2712 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]. Shen CH, et, al. Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model. Br J Pharmacol. 2010 Aug;160(8):2008-27.

    [2]. Pettit GR, et, al. Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41. J Med Chem. 2005 Jun 16;48(12):4087-99.

    [3]. Tozer GM, et, al. Combretastatin A-4 phosphate as a tumor vascular-targeting agent: early effects in tumors and normal tissues. Cancer Res. 1999 Apr 1;59(7):1626-34.

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