型号:
产品价格:电议      采购度:1594      原产地:美洲
发布时间:2021/7/24 1:36:55 所属地区:上海 上海市
简要描述:
Omipalisib (GSK2126458) 是一种口服有效的,高选择性的 PI3K 抑制剂,抑制 p110α/β/δ/γ,mTORC1/2 的活性,Ki 值分别为 nM/ nM/ nM/ nM 和 nM/ nM。Omipalisib 具有抗癌活性。
标签:GSK2126458
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CAS No. : 1086062-66-9
MCE 站:Omipalisib
产品活性:Omipalisib (GSK2126458) 是一种口服有效的,高选择性的 PI3K 抑制剂,抑制 p110α/β/δ/γ,mTORC1/2 的活性,Ki 值分别为 0.019 nM/0.13 nM/0.024 nM/0.06 nM 和 0.18 nM/0.3 nM。Omipalisib 具有抗癌活性。
研究领域:PI3K/Akt/mTOR | Autophagy
In Vitro: Omipalisib (GSK2126458) potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki?of 8 pM, 8 pM and 9 pM, respectively.?Omipalisib causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, Omipalisib (GSK2126458) leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively. The combination of Omipalisib or GSK1120212 with Omipalisib enhances cell growth inhibition and decreases S6 ribosomal protein phosphorylation in drug-resistant clones from the A375 BRAF(V600E) and the YUSIT1 BRAF(V600K) melanoma cell lines.?Omipalisib (GSK2126458) potentiates the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines.
In Vivo: In a BT474 human tumor xenograft model, Omipalisib (GSK2126458) treatment results in a dose-dependent reduction in pAkt-S473 levels, and exhibits dose-dependent tumor growth inhibition at a low dose of 300 μg/kg. Besides, Omipalisib (GSK2126458) shows low blood clearance and good oral bioavailability in four preclinical species (mouse, rat, dog, and monkey).
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical 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 | Glutamine Metabolism 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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更新时间:2024/1/2 10:14:29
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