PI 3-Kα Inhibitor IV-CAS 1188890-32-5-Calbiochem

C₁₆H₁₅N₃O₂S · 2HCl

386.30

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks (IC₅₀ = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC₅₀ ≥ 3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC₅₀ = 580 nM) and serum-stimulated Akt phosphorylation (IC₅₀<3 µM) in A375 melanoma cells.
A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-kinases (IC₅₀ = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC₅₀ ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC₅₀ = 580 nM) and serum-stimulated Akt phosphorylation (IC₅₀<3 µM) in A375 melanoma cells.

Cell permeable: yes
Primary Target
PI 3-Kα
Target IC₅₀: 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively
Product does not compete with ATP.
Reversible: no

Toxicity: Irritant (B)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Hayakawa, M., et al. 2006. Bioorg. Med. Chem.14, 6847.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

off-white

DMSO: 10 mg/mL

ambient

2-8℃

5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1