R1530
作者：齐岳
发布时间：2023-08-25
09:00:21
点击数：
产品名称：R1530
产品描述：
| 产品描述 | R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities. |
| 靶点活性 | VGFR2:10 nM, FGFR1:28 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]. |
| 别名 | R-1530, R 1530 |
| 分子量 | 356.78 |
| 分子式 | C18H14ClFN4O |
| CAS No. | 882531-87-5 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 5 mg/mL (14.01 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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