5.30152

Cdc42/Rac1 Dual Inhibitor, AZA1

• Synonym(e): Cdc42/Rac1 Dual Inhibitor, AZA1, N²,N⁴- bis(2-Methyl-1H-indol-5-yl)pyrimidine-2,4-diamine, Cdc42 Inhibitor IV, Rac1 Inhibitor V
• Empirische Formel (Hill-System): C₂₂H₂₀N₆
• CAS-Nummer: 1071098-42-4
• Molekulargewicht: 368.43
• MDL-Nummer: MFCD31692034
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 25104141
• NACRES: NA.77

Eigenschaften

• Assay: ≥95% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light brown
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: 2-8°C
• SMILES String: CC1=CC2=C(N1)C=CC(=C2)NC3=NC(=NC=C3)NC4=CC5=C(C=C4)NC(=C5)C
• InChI: 1S/C22H20N6/c1-13-9-15-11-17(3-5-19(15)24-13)26-21-7-8-23-22(28-21)27-18-4-6-20-16(12-18)10-14(2)25-20/h3-12,24-25H,1-2H3,(H2,23,26,27,28)

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable