GSK 583

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Cat.No. 6480 - GSK 583 | C20H19FN4O2S | CAS No. 1346547-00-9
Description: Potent RIP2 kinase inhibitor; orally bioavailable and cell permeable
Chemical Name: 6-[(1,1-Dimethylethyl)sulfonyl]-N-(5-fluoro-1H-indazol-3-yl)-4-quinolinamine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent RIP2 kinase inhibitor (IC50 values are 2 and 5 nM at rat and human kinases, respectively). Displays selectivity for RIP2K over p38α, VEGFR2 and a panel of 300 kinases. Exhibits some inhibition at BRK and Aurora A. Also displays similar binding affinity, but no detectable functional activity at RIP3. Active in vivo. Moderately orally bioavailable and cell permeable.

Technical Data

M. Wt 398.45
Formula C20H19FN4O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1346547-00-9
PubChem ID 67469084
InChI Key XLOGLWKOHPIJLV-UHFFFAOYSA-N
Smiles CC(C)(S(=O)(C1=CC2=C(N=CC=C2NC3=NNC4=CC=C(C=C34)F)C=C1)=O)C

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.84 100
ethanol 7.97 20

Preparing Stock Solutions

The following data is based on the product molecular weight 398.45. 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 2.51 mL 12.55 mL 25.1 mL
5 mM 0.5 mL 2.51 mL 5.02 mL
10 mM 0.25 mL 1.25 mL 2.51 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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References

References are publications that support the biological activity of the product.

Haile et al (2016) The identification and pharmacological characterization of 6-(tert-butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a highly potent and selective inhibitor of RIP2 kinase. J.Med.Chem. 59 4867 PMID: 27109867


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Keywords: GSK 583, GSK 583 supplier, GSK583, Potent, RIP2, kinase, inhibitors, inhibits, oral, bioavailability, cell, permeable, receptor-interacting, protein, 1, Other, Kinases, 6480, Tocris Bioscience

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