PKC412 #9493

Product Usage Information

PKC412 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 1 mg in 175.24 μL DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 0.1-10 μM for 18-48 hours. Soluble in DMSO at 100 mg/mL; soluble in ethanol at 5 mg/mL with warming; very poorly soluble in water with maximum solubility estimated to be about 10-20 μM.

Storage:

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight:

570.65 g/mol

Purity:

>99%

Molecular Formula:

C₃₅H₃₀N₄O₄

Background

The staurosporine analog, PKC412, inhibits a variety of serine/threonine and tyrosine kinases including PKC (IC₅₀ = 50 nM), cyclic AMP-dependent protein kinase (IC₅₀ = 2.4 µM), S6 kinase (IC₅₀ = 5.0 µM), and EGFR (epidermal growth factor receptor) tyrosine kinase activity (IC₅₀ = 3.0 µM) (1). PKC412 has also demonstrated stong inhibitory effects on FLT3, which causes G1 cell cycle arrest and apoptosis (2).

1. Meyer, T. et al. (1989) Int J Cancer 43, 851-6.
2. Bali, P. et al. (2004) Clin Cancer Res 10, 4991-7.