AMG 511 |
カタログ番号GC39695 |
AMG 511 は、PI3Kα、β、δ、およびγに対してそれぞれ 4 nM、6 nM、2 nM、および 1 nM の Ki を持つ、クラス I PI3K の強力な経口利用可能な汎阻害剤です。 AMG 511 は、p-Akt (Ser473) の減少によって示される PI3K シグナル伝達を大幅に抑制します。 AMG 511 は、マウス膠芽腫異種移植モデルで抗腫瘍活性を示します。
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Cas No.: 1253573-53-3
Sample solution is provided at 25 µL, 10mM.
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model[1].
[1]. Mark H Norman, et al. Selective Class I Phosphoinositide 3-kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511. J Med Chem. 2012 Sep 13;55(17):7796-816.
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