Non disponible en dehors du Royaume-Uni et de l'Irlande
Biochem/physiol Actions
Reversible: yes
Product competes with ATP.
Target IC50: 22 nM, 50 nM, 86 nM, 95 nM, 160 nM, 330 nM, 390 nM, 528 nM, 570 nM, 570 nM, 600 nM, 790 nM, 800 nM, 912 nM, and 1.0 µM against primary targets in the order listed
Cell permeable: yes
Primary TargetPKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR
General description
A cell-permeable Staurosporine (Cat. No. 569397) derivative that displays antitumor properties. Acts as a broad-spectrum, reversible, and ATP-competitive inhibitor of PKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR (IC50 = 22 nM, 50 nM, 86 nM, 95 nM, 160 nM, 330 nM, 390 nM, 528 nM, 570 nM, 570 nM, 600 nM, 790 nM, 800 nM, 912 nM, and 1.0 µM, respectively). At higher concentrations, also inhibits Ins-R and IGF-1R (IC50 = 10 µM). Shown to potently inhibit the proliferation of Ba/F3 cells expressing constitutively active Flt3 (IC50﹤10 nM).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Weisberg, E., et al. 2002. Cancer Cell1, 433.Fabbro, D., et al. 2000. Anticancer Drug Des.15, 17.Meyer, T., et al. 1999. Int. J. Cancer81, 669.Meyer, T., et al. 1989. Int. J. Cancer43, 851.
Packaging
1 mg in Plastic ampoule
Packaged under inert gas
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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