| Identification | Back Directory | [Name]
4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile | [CAS]
871307-18-5 | [Synonyms]
TC-S 7006
Tpl2-IN-2p
Tpl2 Kinase Inhibitor
Tpl2 Kinase Inhibitor 1
4-(3-chloro-4-fluorophenylamino)-6-(pyridin-3-ylmethylamino)-1,7-naphthyridine-3-carbonitrile
4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile
1,7-Naphthyridine-3-carbonitrile, 4-[(3-chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]- | [Molecular Formula]
C21H14ClFN6 | [MOL File]
871307-18-5.mol | [Molecular Weight]
404.83 |
| Chemical Properties | Back Directory | [Boiling point ]
616.3±55.0 °C(Predicted) | [density ]
1.45 | [storage temp. ]
Sealed in dry,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 |
| Hazard Information | Back Directory | [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 |
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