Chemical Name: 5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine
Biological ActivityMulti-kinase inhibitor. Exhibits inhibitory activity against Chk2, KDR, FGFR, Aurora A kinase and Cdk2 (IC50 values are 24, 34, 50, 58 and 88 nM respectively). Also binds VEGFR-2, FGFR1 and PDGFRβ (Kd values are 0.015, 0.061 and 0.088 μM respectively). Displays antiproliferative activity in vitro; inhibits mitosis and angiogenesis. Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: implications for therapy.
Tovar et al.
Cell Cycle, 2010;9:3364
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor R1530 for the treatment of solid tumors.
Liu et al.
ACS Med.Chem.Lett., 2013;4:259
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