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Submit ReviewR 1530
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% (HPLC)
Biological Activity for R 1530
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 for R 1530
| M. Wt | 356.78 |
| Formula | C18H14ClFN4O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 882531-87-5 |
| PubChem ID | 11610113 |
| InChI Key | UOVCGJXDGOGOCZ-UHFFFAOYSA-N |
| Smiles | FC(C(OC)=C1)=CC2=C1NC3=NNC(C)=C3N=C2C4=C(Cl)C=CC=C4 |
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.
Product Datasheets for R 1530
References for R 1530
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
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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
Citations for R 1530
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