R1530
Cat. No.:YN440289
产品名称: | R1530 |
CAS No.: | 882531-87-5 |
Chemical Name: | 5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-pyrazolo[3,4-b][1,4]benzodiazepine |
Synonyms: | R-1530,R 1530 |
分子量: | 356.78 |
分子式: | C₁₈H₁₄ClFN₄O |
SMILES: | CC(NN1)=C2C1=NC3=CC(OC)=C(F)C=C3C(C4=CC=CC=C4Cl)=N2 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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VGFR2、FGFR1作用的IC50分别为 10 nM 和 28 nM。 |
IC50和靶点: | [{name:"KDR:10 nM (IC50)"},{name: "FGFR1:28 nM (IC50)"}] |
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Liu, J.-J., Higgins, B., Ju, G., et al.Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumorsACS Med. Chem. Lett.4(2),259-263(2013)
Tovar, C., Higgins, B., Deo, D.D., et al.Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapyCell Cycle9(16),3364-3375(2010)
Kolinsky, K., Tovar, C., Zhang, Y.-E., et al.Preclinical evaluation of the novel multi-targeted agent R1530Cancer Chemother. Pharmacol.68(6),1585-1594(2011)