CDC42/RAC1 DUAL INHIBITOR A 1PC X 10MG (C15-1305-007)

General description

A cell-permeable indolylpyrimidinediamine compound that selectively suppresses cellular levels of GTP-bound Rac1 and Cdc42, but not RhoA, in serum-starved prostate cancer cultures upon EGF-stimulation (% of non-stimulated control Rac1-GTP level with/without 20 µM AZA1 = 56/375 in 22Rv1, 30/235 in DU 154, and 12/118 in PC-3 cells; % of non-EGF-stimulated control Cdc42-GTP level with/without 20 µM AZA1 = 15/170 in 22Rv1, 30/105 in DU 154, and 12/100 in PC-3 cells), resulting in effective suppression of PAK1, Akt, and BAD phosphorylations, as well as time- and dose-dependent (2 to 10 µM and up to 72 hr) growth inhibition of the cells in serum-deprived cultures with or without EGF stimulation. Dual Cdc42/Rac1 inhibition by AZA1 also effectively inhibits prostate cancer cells migration by decreasing cellular F-/G-actin ratio and disabling both filopodia and lamepodia formation. Daily intraperitoneal injection (100 µg/100 µL 30% DMSO/mouse) is shown to be efficacious in suppressing 22Rv1 tumor expansion in mice in vivo.

A cell-permeable indolylpyrimidinediamine compound that selectively suppresses upregulation of GTP-bound Rac1 and Cdc42, but not RhoA, in prostate cancer cells upon EGF-stimulation (Effec. Conc. = 20 µM in serum-starved 22Rv1, DU 154, PC-3 cultures), resulting in time- and dose-dependent (2 to 10 µM and up to 72 h) growth inhibition in serum-deprived cultures with or without EGF stimulation. Dual Cdc42/Rac1 inhibition by AZA1 also effectively inhibits prostate cancer cells migration by decreasing cellular F-/G-actin ratio and disabling both filopodia and lamepodia formation. Daily intraperitoneal injection (100 µg/100 µL 30% DMSO/mouse) is shown to suppress 22Rv1 tumor expansion in mice in vivo.

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

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

Zins, K., et al. 2013. PLoS One8, e74924.

Legal Information

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

Molecular Weight: 368.43. Empirical Formula: C₂₂H₂₀N₆. Assay: ≥. 95% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: light brown. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. SMILES string: CC1: CC2: C(N1)C: CC(: C2)NC3: NC(: NC: C3)NC4: CC5: C(C: C4)NC(: C5)C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.