R 1530

Pricing Availability   Qty
Cat.No. 4885 - R 1530 | C18H14ClFN4O | CAS No. 882531-87-5
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)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.68 100
ethanol 35.68 100

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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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View all Other RTKs Inhibitors

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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