R 1530

Cat. No. 4885

R 1530 C18H14ClFN4O [882531-87-5]

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Chemical Name: 5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine

Biological Activity

Multi-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.

Technical Data

M.Wt:
356.78
Formula:
C18H14ClFN4O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
882531-87-5

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Liu et al (2013) Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor R1530 for the treatment of solid tumors. ACS Med.Chem.Lett. 4 259.

Tovar et al (2010) Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: implications for therapy. Cell Cycle 9 3364. PMID: 20814247.

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Keywords: R 1530, supplier, R1530, multi-RTK, inhibitors, inhibits, receptor, tyrosine, kinases, Chk2, KDR, FGFR, Aurora, A, Cdk2, VEGFR-2, FGFR1, PDGFRb, PDGFRbeta, PDGFRβ, angiogenesis, antiangiogenics, Tocris Bioscience, Other RTKs Inhibitor products

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