882531-87-5
Chemical Structure
R1530
- CAS No.: 882531-87-5
- Formula:C18H14ClFN4O
- Molecular Weight:356.78
IUPAC Name: 5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydrobenzo[e]pyrazolo[4,3-b][1,4]diazepine
InChIKey: UOVCGJXDGOGOCZ-UHFFFAOYSA-N
SMILES: CC(NN1)=C2C1=NC3=CC(OC)=C(F)C=C3C(C4=CC=CC=C4Cl)=N2
Biological Activity: R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence[1][2].
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R1530 | 98.29% | R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence. | ||||||||||||||||||||
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References
- [1]. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263. [Content Brief]
- [2]. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75. [Content Brief]
