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GNE-493

CAS No. : 1033735-94-2

MCE 站：GNE-493

产品活性：GNE-493 是一种有效的，选择性的 PI3K/mTOR 抑制剂，抑制 PI3Kα，PI3Kβ，PI3Kδ，PI3Kγ 和 mTOR。IC₅₀ 为 3.4 nM，12 nM，16 nM，16 nM 和 32 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K  |  mTOR

In Vitro: GNE-493 is a low molecular weight, potent dual inhibitor of pan-PI3 kinases and mTOR. GNE-493 displays approximately equipotent inhibition of Class I PI3K isoforms, is submitted for screening in a 142 kinase panel provided by Invitrogen’s SelectScreen service. Of these kinases, only three are subject to greater than 50% inhibition by GNE-493, and are inhibited greater than 80% when tested at 1 μM. Subsequently measured IC50s demonstrated that GNE-493 is more than 100-fold selective for PI3Kα over these three unrelated kinases (Aurora A IC₅₀>10 μM, MLK1 IC₅₀=591 nM and SYK IC₅₀=371 nM).

In Vivo: To confirm and compare in vivo efficacy, GNE-493 is examined in the human MCF7.1 breast cancer xenograft model that harbors a PI3Kα activating mutation. Mice bearing xenografts are dosed orally once daily with 10 mg/kg of GNE-493 for 21 continuous days. Similar to observations made in the PC3 prostate cancer xenograft model, 10 mg/kg of GNE-493 results in 73% tumor growth inhibition at day 21 when compared to vehicle control animals. When achieving comparable levels of drug exposure, GNE-493 shows a similar suppression of the PI3K pathway and consequently, a similar efficacy profile against MCF7.1 breast tumors.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Antioxidants Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Rapamycin  |  3-Methyladenine  |  LY294002  |  Wortmannin  |  Everolimus  |  MHY1485  |  Quercetin  |  740 Y-P  |  3BDO  |  Temsirolimus  |  Salidroside  |  Torkinib  |  PI-103  |  D-α-Hydroxyglutaric acid disodium  |  Isorhamnetin  |  L-Leucine  |  Recilisib  |  Autophinib  |  Dihydromyricetin  |  AZD 6482  |  PI3K-IN-1  |  TG100-115  |  α-Linolenic acid  |  TGX-221  |  1-Deoxynojirimycin  |  YS-49  |  AS-605240  |  PKI-402  |  Disitertide  |  Erucic acid

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