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R 1530

Catalog #: 4885 Datasheet / COA / SDS

Discontinued Product

4885 has been discontinued.
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R 1530 | CAS No. 882531-87-5 | Additional RTK Inhibitors
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Description: Multi-RTK inhibitor; inhibits angiogenesis

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

Purity: ≥98%

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Biological Activity

R 1530 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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
  2. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: implications for therapy.
    Tovar et al.
    Cell Cycle, 2010;9:3364

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