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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 356.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.8 mL||14.01 mL||28.03 mL|
|5 mM||0.56 mL||2.8 mL||5.61 mL|
|10 mM||0.28 mL||1.4 mL||2.8 mL|
|50 mM||0.06 mL||0.28 mL||0.56 mL|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for R 1530, please let us know.
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Keywords: R 1530, 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, Other, RTKs, Antiangiogenics, 4885, Tocris Bioscience
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