4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile Chemical Properties

Boiling point:

616.3±55.0 °C(Predicted)

Density 

1.45

storage temp. 

2-8°C

solubility 

DMF: 1 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 1 mg/ml

form 

A crystalline solid

pka

4.80±0.10(Predicted)

color 

Yellow to green

4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile Usage And Synthesis

Description

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC₅₀ = 0.05 μM). It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC₅₀s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC₅₀s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by 1,25-dihydroxy vitamin D₃ (calcitriol; ) in HL-60 and U937 leukemia cells when used at a concentration of 5 μM. Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.

Uses

TC-S 7006 is a Tpl2 kinase inhibitor.

IC 50

MAP3K8; p38: 180 μM (IC₅₀); MK2: 110 μM (IC₅₀)

storage

Store at -20°C

References

[1] NEAL GREEN  et al. et al. Inhibition of Tpl2 Kinase and TNF-α Production with 1,7-Naphthyridine-3-carbonitriles: Synthesis and Structure—Activity Relationships.[J]. ChemInform, 2006, 37 9. DOI: 10.1002/chin.200609160
[2] XUENING WANG  George P S. Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cells[J]. Journal of Steroid Biochemistry and Molecular Biology, 2010, 121 1: Pages 395-398. DOI: 10.1016/j.jsbmb.2010.03.016
[3] XUENING WANG. Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D(3).[J]. Cell Cycle, 2010, 9 22: 4542-4551. DOI: 10.4161/cc.9.22.13790

4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile(871307-18-5)Related Product Information

• 3-Aminopyridine
• 2-Aminopyridine
• Glycine
• 4-Dimethylaminopyridine
• ALTRENOGEST
• CHLOROPHENYLSILANE
• 4,4'-DDT
• 3,4'-DIAMINODIPHENYLMETHANE
• AMINO ACIDS
• Difluorochloromethane
• 3-Chloro-4-fluoroaniline
• 4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile