A cell-permeable indenopyrazole compound that displays potent antiproliferative properties in several human tumor cell lines (IC50<33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC50 = 4.2 nM and 45 nM for -β and -α, respectively) and c-Abl (IC50 = 22 nM). Exhibits less activity towards Lck, c-Src, and Fyn (IC50 = 100 nM, 185 nM and 378 nM, respectively) and exhibits little or no inhibition toward VEGFR, HER-2, Cdk′s-1,-2,-4 &-7, bFGFR-1 and EGFR (IC50 = 3.1 µM, >10 µM, >10 µM, 45.8 µM and >100 µM, respectively).
Actions biochimiques/physiologiques
Cell permeable: yes
Primary Target PDGFR Tyrosine Kinase
Product competes with ATP.
Reversible: yes
Target IC50: 4.2 nM and 45 nM for -β and -α form of PDGFR, respectively
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Harmful (C)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Autres remarques
Ho, C.Y., et al. 2005. J. Med. Chem.48, 8163.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
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