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
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 Basic information
- Product 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
- Synonyms:
-
- 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
- 8-Chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethylpiperidin-4-yl)-1H-1,2,3-triazol-4-yl]methyl]amino]quinoline-3-carbonitrile
- Cot inhibitor-2
- 3-Quinolinecarbonitrile, 8-chloro-4-[(3-chloro-4-fluorophenyl)aMino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1,2,3-triazol-4-yl]Methyl]aMino]-
- 8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1
- COT INHIBITOR2; COT INHIBITOR 2
- Tpl2-IN-34
- KIN001-266
- CAS:
- 915363-56-3
- MF:
- C26H25Cl2FN8
- MW:
- 539.43
- Mol File:
- 915363-56-3.mol
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 Chemical Properties
- Boiling point:
- 713.3±70.0 °C(Predicted)
- Density
- 1.45
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 100 mg/mL (185.38 mM)
- pka
- 8.62±0.10(Predicted)
- form
- Powder
- color
- Light yellow to green yellow
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 Usage And Synthesis
Uses
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM[1].
Definition
ChEBI: 8-chloro-4-(3-chloro-4-fluoroanilino)-6-[[1-(1-ethyl-4-piperidinyl)-4-triazolyl]methylamino]-3-quinolinecarbonitrile is an aminoquinoline.
in vivo
Cot inhibitor-2 (compound 34) is orally administered in rats with 100 mg/kg dosing and showed a Cmax of 517 ng/mL (0.89 μM) and AUC of 4841 ng h/mL. Cot inhibitor-2 is tested in the LPS-induced TNF-α production model in female Sprague-Dawley rats. With a 25 mg/kg po dose, Cot inhibitor-2 inhibits LPS-induced TNF-α production by 83%[1].
storage
Store at -20°C
References
[1] Junjun Wu, et al. 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 Jul 1;19(13):3485-8. DOI:10.1016/j.bmcl.2009.05.009
8-Chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1,2,3-triazol-4-yl]methyl]amino]-3-QuinolinecarbonitrileSupplier
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