Powder: -20°C for 3 years | In solvent: -80°C for 1 year
R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 48.00 | |
2 mg | In stock | $ 68.00 | |
5 mg | In stock | $ 113.00 | |
10 mg | In stock | $ 172.00 | |
25 mg | In stock | $ 347.00 | |
50 mg | In stock | $ 592.00 | |
100 mg | In stock | $ 852.00 |
Description | R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities. |
Targets&IC50 | VGFR2:10 nM, FGFR1:28 nM |
In vitro | 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]. |
In vivo | 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]. |
Synonyms | R-1530, R 1530 |
Molecular Weight | 356.78 |
Formula | C18H14ClFN4O |
CAS No. | 882531-87-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5 mg/mL (14.01 mM)
You can also refer to dose conversion for different animals. More
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R1530 882531-87-5 Angiogenesis Tyrosine Kinase/Adaptors FGFR VEGFR FLT PDGFR antitumor Inhibitor Fibroblast growth factor receptor mitosis angiogenesis R-1530 R 1530 antiproliferative Apoptosis inhibit mitotic Vascular endothelial growth factor receptor inhibitor