R-1530
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CAS No. | 882531-87-5 | Cat. No. | BCP13142 |
Name | R-1530 | ||
Synonyms | R 1530;R1530; | ||
SMILES | |||
Chemical Name | |||
Formula | C18H14ClFN4O | M. Wt | 356.78 |
Purity | 98% | Storage | Store at 4-8°C |
Description | R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis. in vitro: 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 thus supporting the rationale for cancer therapy by induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition . R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial |
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