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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)
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 Data 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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Product Datasheets for KIN001-266
References for KIN001-266
References are publications that support the biological activity of the product.
Glatthar et al (2016) Discovery of imidazoquinolines as a novel class of potent, selective, and in vivo efficacious Cancer Osaka Thyroid (COT) kinase inhibitors. J.Med.Chem. 59 7544 PMID: 27502541
Wu et al (2009) Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. Bioorg.Med.Chem.Lett. 19 3485 PMID: 19464884
If you know of a relevant reference for KIN001-266, please let us know.
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Keywords: KIN001-266, KIN001-266 supplier, potent, selective, TPL2, Cot, MAP3K8, inhibits, inhibitors, orally, bioavailable, Other, MAPK, 6984, Tocris Bioscience
Citations for KIN001-266
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.