KIN001-266

Key Product Details

Product Description

KIN001-266 is a potent and selective Tpl2 (Cot; MAP3K8) inhibitor (IC₅₀ = 1.6 nM). It exhibits 6875-fold selectivity over EGFR. In vivo, it inhibits TNF-α production in a LPS-stimulated rat inflammation model. KIN001-266 is orally bioavailable.

Product Specifications for KIN001-266

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for KIN001-266

The following data is based on the product molecular weight 539.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.85 mL	9.27 mL	18.54 mL
5 mM	0.37 mL	1.85 mL	3.71 mL
10 mM	0.19 mL	0.93 mL	1.85 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

Calculators

Background References

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

• Wu Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. Bioorg.Med.Chem.Lett. 2009 PMID: 19464884
• Glatthar Discovery of imidazoquinolines as a novel class of potent, selective, and in vivo efficacious Cancer Osaka Thyroid (COT) kinase inhibitors. J.Med.Chem. 2016 PMID: 27502541

Product Documents for KIN001-266