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Tpl2-1

Chemical Structure : Tpl2-1

CAS No.: 871307-18-5

Tpl2-1 (Tpl2 kinase inhibitor 1, Cot/MAP3K8 inhibitor, Tpl2-IN-2p)

Catalog No.: PC-70030Not For Human Use, Lab Use Only.

Tpl2-1 is a potent, selective, reversible and ATP-competitive inhibitor of Tpl2 kinase (Cot/MAP3K8) with IC50 of 50 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Tpl2-1 is a potent, selective, reversible and ATP-competitive inhibitor of Tpl2 kinase (Cot/MAP3K8) with IC50 of 50 nM.
Tpl2-1 dispalys significant selectivity over other related kinases (IC50= 5, >40, 110, 180, >400 and >400 uM for EGFR, MEK, MK2, p38, Src, and PKC, respectively).
Tpl2-1 inhibits LPS-induced TNF-α production both from primary human monocytes and in whole blood with IC50 of 0.7 and 8.5 uM, respectively;

Physicochemical Properties

M.Wt 404.83
Formula C21H14ClFN6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((3-chloro-4-fluorophenyl)amino)-6-((pyridin-3-ylmethyl)amino)-1,7-naphthyridine-3-carbonitrile

References

1. Gavrin LK, et al. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92.

2. Lee WJ, et al. Neoplasia. 2013 Sep;15(9):1036-48.

3. Lee HW, et al. Mol Cancer Res. 2013 Nov;11(11):1375-86.

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