化合物R1530 TQ0317

Product Introduction
Bioactivity


英文名: R1530

描述: R1530 是一种多激酶抑制剂，具有抗肿瘤和抗血管生成活性。它是具有口服活性的有丝分裂/血管生成高效双重作用抑制剂， 抑制 VGFR2、FGFR1作用的 IC50分别为 10 nM 和 28 nM。

体外活性: R1530 inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as VEGFR-1/2/3, PDGFR, Flt-3, and FGFR-1/2. In the presence of R1530, polyploid cancer cells underwent apoptosis or became senescent which translated into potent in vitro and in vivo efficacy. Normal proliferating cells were resistant to R1530-induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition [1]. R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial and fibroblast cells was also inhibited [2].

体内活性: Showing significant tumor growth inhibition in a lung cancer xenograft model, R1530 was administered at doses ranging from once daily, weekly and twice weekly (3.125-50 mg/kg qd, 100 mg/kg qw, 100 mg/kg kg biw). Tumor regression occurred in all models treated with the maximum tolerated daily dose (50 mg/kg). Doses of 25 and 50 mg/kg qd resulted in biologically significant increases in survival in all models tested. After oral administration to nude mice, R1530 showed good tissue permeability. Exposure was dose-dependent, up to 100 mg/kg when administered orally[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 5 mg/mL (14.01 mM)


关键字: antitumor | Inhibitor | Fibroblast growth factor receptor | mitosis | FGFR | angiogenesis | R1530 | VEGFR | antiproliferative | Apoptosis | inhibit | mitotic | Vascular endothelial growth factor receptor

相关产品: δ-Tocotrienol | CP-547632 | Oglufanide | hCA/VEGFR-2-IN-4 | Bevacizumab | OSI-930 | Golvatinib | SU5214 | BGB-102 | Xanthatin

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Osteogenesis Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途