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Submit ReviewKIN001-266
说明： Potent and selective Tpl2 (MAP3K8) inhibitor
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for KIN001-266
| 分子量 | 539.44 |
| 公式 | C26H25Cl2FN8 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for KIN001-266
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 53.94 | 100 | |
| ethanol | 10.79 | 20 |
制备储备液 for KIN001-266
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for KIN001-266
参考文献 for KIN001-266
参考文献是支持产品生物活性的出版物。
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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关键词: KIN001-266, KIN001-266 supplier, potent, selective, TPL2, Cot, MAP3K8, inhibits, inhibitors, orally, bioavailable, Other, MAPK, 6984, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.