PI 3-Kalpha Inhibitor IV MF: C16H15N3O2S 2HCl
MW: 386.3
A potent and isoform-selective inhibitor of the PI 3-kinase family.

PI 3-Kα Inhibitor IV

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应用; PI 3-Kα Inhibitor IV is a potent and isoform-selective inhibitor of the PI 3-kinase family
分子量: 386.3
分子式: C16H15N3O2S 2HCl
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

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.


参考文献

1. Hayakawa, M., et al. 2006. Bioorg. Med. Chem. 14: 6847-6858. PMID: 16837202

物理状态 :
Solid
溶解度 :
Soluble in DMSO (10 mg/ml).
保存 :
Store at 4° C
沸点 :
513.9° C at 760 mmHg (Predicted)
折射率 :
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)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
SMILES :
C1COCCN1C2=NC(=NC3=C2SC=C3)C4=CC(=CC=C4)O.Cl.Cl

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引用1 - 11

PMID: # 22335196  Wang, J. et al. 2012. J. Pineal Res. 53: 77-90.

引用1 - 11
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