General description
A cell-permeable 5-phenyl-2-thiazolamine compound that acts as a potent, ATP binding site-targeting inhibitor of Flt3 (IC50 = 50 nM). It inhibits c-Kit, KDR, c-Abl, Cdk1, c-Src, and Tie-2 only at much higher concentrations (IC50 = 0.26, 0.91, 1.2, 2.1, 2.8, and 8.0 µM, respectively) and exhibits little activity against a panel of 12 other commonly studied kinases even at concentrations as high as 10 µM. Blocks FLT3-dependent cell proliferation in a dose-dependent manner (IC50 = 52, 240, and 760 nM in MV4:11-ITD, BaF3-ITD, and BaF3-D835/Y cells).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Flt-3
Product competes with ATP.
Reversible: no
Target IC50: 50 nM against Flt3
Packaging
Packaged under inert gas
Warning
Toxicity: Harmful (C)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Furet, P., et al. 2006. J. Med. Chem.49, 4451.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51284302
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 343022-5MG