TL4-12

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Cat.No. 5910 - TL4-12 | C25H27F3N6O2 | CAS No. 1620820-12-3
Description: Potent MAP4K2 (GCK) inhibitor
Chemical Name: 4-Methyl-3-[[6-(methylamino)-4-pyrimidinyl]oxy]-N-[3-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent MAP4K2 (GCK) inhibitor (IC50 = 37 nM). Exhibits >70-fold selectivity for MAP4K2 over TAK1 (IC50 = 2.7 μM for TAK1). Inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation, in vitro.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M. Wt 500.53
Formula C25H27F3N6O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1620820-12-3
Smiles O=C(C1=CC=C(C)C(OC2=CC(NC)=NC=N2)=C1)NC3=CC(N4CCN(C)CC4)=CC(C(F)(F)F)=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.01 20
1eq. HCl 10.01 20

Preparing Stock Solutions

The following data is based on the product molecular weight 500.53. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2 mL 9.99 mL 19.98 mL
5 mM 0.4 mL 2 mL 4 mL
10 mM 0.2 mL 1 mL 2 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

Tan et al (2015) Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J.Med.Chem. 58 183 PMID: 25075558


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Literature in this Area

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MAPK Signaling Scientific Review

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