R1530

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

R1530  纯度: 99.06%

R1530 是一种高效的,具有口服活性的有丝分裂/血管生成 (mitosis/angiogenesis) 双重作用抑制剂,具有抗肿瘤和抗血管生成活性。R1530 是一种多激酶抑制剂,与 31 种激酶结合的 Kd 均小于 500 nM。R1530 抑制 VGFR2FGFR1 作用的 IC50 分别为 10 nM 和 28 nM。

R1530

R1530 Chemical Structure

CAS No. : 882531-87-5

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R1530 相关产品

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生物活性

R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kds of <500 nm. r1530 inhibits VGFR2 and FGFR1 with IC50s of 10 nM and 28 nM, respectively[1][2][3].

IC50 & Target[1]

KDR

10 nM (IC50)

FGFR1

28 nM (IC50)

分子量

356.78

Formula

C18H14ClFN4O

CAS 号

882531-87-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 2 mg/mL (5.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8028 mL 14.0142 mL 28.0285 mL
5 mM 0.5606 mL 2.8028 mL 5.6057 mL
10 mM

*

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。-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]. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263.

    [2]. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75.

    [3]. Kolinsky K, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.

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