STAUROSPORINE N-BENZOYL 1PC X 1MG

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 &microM). Shown to potently inhibit the proliferation of Ba/F3 cells expressing constitutively active Flt3 (IC₅₀<10 nM).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
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

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany