KIN001-266

Name: KIN001-266
Brand: Tocris Bioscience
SKU: 6984

Tocris Bioscience, part of Bio-Techne | Catalog # 6984

COA / SDS

Potent and selective Tpl2 (MAP3K8) inhibitor

Key Product Details

Description:	Potent and selective Tpl2 (MAP3K8) inhibitor
Chemical Name:	8-Chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1,2,3-triazol-4-yl]methyl]amino]-3-quinolinecarbonitrile
Purity:	≥98% (HPLC)
Molecular Weight:	539.44

View Full Technical Details for KIN001-266

Technical Data
Citations

Biological Activity for KIN001-266

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.

Technical Data for KIN001-266

M. Wt	539.44
Formula	C₂₆H₂₅Cl₂FN₈
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	915363-56-3
PubChem ID	44143370
InChi Key	PHNZIIMWDVXPGG-UHFFFAOYSA-N
Smiles	CCN1CCC(N2C=C(N=N2)CNC3=CC4=C(C(Cl)=C3)N=CC(C#N)=C4NC5=CC(Cl)=C(C=C5)F)CC1

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 for KIN001-266

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	53.94	100
	ethanol	10.79	20

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for KIN001-266

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