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Miransertib
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Miransertib
CAS No. : 1313881-70-7
MCE 站:Miransertib
产品活性:Miransertib (ARQ-092) 是一种有效的,具有口服活性的,选择性和变构性 Akt 抑制剂,对 Akt1,Akt2,Akt3 的 IC50 分别为 2.7 nM,14 nM 和 8.1 nM。Miransertib 还是有效的 AKT1-E17K 突变蛋白抑制剂,并可用于 PI3K/AKT 驱动的肿瘤和 Proteus 综合征的研究。Miransertib 有效抑制利什曼原虫 (Leishmania)。
研究领域:PI3K/Akt/mTOR | Anti-infection
In Vitro: In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells. The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC50=0.31 μM).
Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis-infected macrophages. Miransertib also enhances mTOR dependent autophagy in Leishmania-infected macrophages[2]
In Vivo: Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t1/2 values of 17 h in rats versus 7 h in monkeys. The Cmax is 198 ng/mL and 258 ng/mL and the AUCinf was 5496 h•ng/mL and 2960 h•ng/mL in rats and monkeys, respectively.
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Anti-Infection Compound Library | 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 | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active 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 | Antiparasitic Compound library | Angiogenesis Related Compound Library | Chloroquine | MK-2206 dihydrochloride | SC79 | Hydroxychloroquine sulfate | Capivasertib | Ipatasertib | Kaempferol | Ivermectin | Honokiol | Metronidazole | Dihydroartemisinin | Niclosamide | Suramin sodium salt | Artesunate | GSK-690693 | AKT inhibitor VIII | Artemisinin | Quinidine | Oridonin | Halofugi | Perifosine | Guggulsterone | Obatoclax Mesylate | RRx-001 | Recilisib | Afuresertib | Triciribine | Mefloquine hydrochloride | Sanguinarine chloride
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