PI 3-Kα Inhibitor IV
Application
PI 3-Kα Inhibitor IV is a potent and isoform-selective inhibitor of the PI 3-kinase family
분자량:
386.3
분자식:
C16H15N3O2S 2HCl
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
PI 3-Kα Inhibitor IV is a cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of the PI 3-kinase family (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for PI 3-kinase p110 α (p110α), PI 3-kinase p110 β (p110β), p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-kinase targets only at much higher concentrations (IC50 ≥3.4 μM for Cdk2/E, KDR, PKA, and PKCα). PI 3-Kα Inhibitor IV has been shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50 <3 μM) in A375 melanoma cells.
References
1. Hayakawa, M., et al. 2006. Bioorg. Med. Chem. 14: 6847-6858. PMID: 16837202
Physical State
:
Solid
용해도
:
Soluble in DMSO (10 mg/ml).
저장
:
Store at 4° C
비등점
:
513.9° C at 760 mmHg (Predicted)
굴절률
:
n20D ~1.69 (Predicted)
IC50
:
p110α: IC50 = 2 nM; p110β: IC50 = 16 nM; p110γ: IC50 = 660 nM; PI 3-K C2β: IC50 = 220 nM; Cdk2/E: IC50 = ≥3.4 µM; KDR: IC50 = ≥3.4 µM; PKA: IC50 = ≥3.4 µM; PKCα: IC50 = ≥3.4 µM; Cell proliferation: IC50 = 580 nM (A375 melanoma cells); Serum-stimulated Akt phosphorylation: IC50 = <3 µM (A375 melanoma cells)
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
PubChem CID
:
SMILES
:
C1COCCN1C2=NC(=NC3=C2SC=C3)C4=CC(=CC=C4)O.Cl.Cl
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