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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Polo-like Kinase (PLK)-R1530
R1530

Chemical Structure : R1530

CAS No.: 882531-87-5

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R1530 (R-1530)

货号: PC-28544Not For Human Use, Lab Use Only.

R1530 (R-1530) is a highly potent, orally active mitosis/angiogenesis inhibitor, inhibits angiogenesis-related receptor tyrosine kinases (KDR, FGFR) with IC50 of 10 nM and 28 nM, also inhibits PLK4 with IC50 of 7.06 nM.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

R1530 (R-1530) is a highly potent, orally active mitosis/angiogenesis inhibitor, inhibits angiogenesis-related receptor tyrosine kinases (KDR, FGFR) with IC50 of 10 nM and 28 nM, also inhibits PLK4 with IC50 of 7.06 nM.
R1530 shows much weaker activities against CDK2 and CDK4.
R1530 inhibits the kinase activities of vascular endothelial growth factor receptor 2 (VGFr2), FGFR1, and PDGFR-β.
R1530 exhibits potent in vitro antiproliferative activity in various human tumor tissues including breast, colon, lung, prostate, melanoma, and oral epidermoid (IC50= 0.2-3.4 μM).
R1530 (25 or 50 mg/kg) produced significant tumor growth inhibition in MDA-MB-435 human tumor xenograft model.

物理化学性质&存储条件

分子量 356.79
分子式 C18H14ClFN4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-(2-Chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydrobenzo[e]pyrazolo[4,3-b][1,4]diazepine

参考文献

1. Liu JJ, et al. ACS Med Chem Lett. 2013 Jan 15;4(2):259-63.

2. Kolinsky K, et al. Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.

3. Tovar C, et al. Cell Cycle. 2010 Aug 15;9(16):3364-75.

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