MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Miransertib hydrochloride

CAS No. : 1313883-00-9

MCE 站：Miransertib hydrochloride

产品活性：Miransertib hydrochloride (ARQ-092 hydrochloride) 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 hydrochloride 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 hydrochloride 有效抑制利什曼原虫 (Leishmania)。

研究领域：PI3K/Akt/mTOR  |  Anti-infection

作用靶点：Akt  |  Parasite

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 t_1/2 values of 17 h in rats versus 7 h in monkeys. The C_max is 198 ng/mL and 258 ng/mL and the AUC_inf 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：Chloroquine  |  Hydroxychloroquine sulfate  |  Ivermectin  |  Honokiol  |  Kaempferol  |  Metronidazole  |  Dihydroartemisinin  |  Niclosamide  |  Suramin sodium salt  |  Artesunate  |  GSK-690693  |  Artemisinin  |  Quinidine  |  Oridonin  |  Perifosine  |  Guggulsterone  |  Halofuginone  |  Miransertib  |  Triciribine  |  Mefloquine hydrochloride  |  Quinacrine dihydrochloride  |  Sanguinarine chloride  |  Recilisib  |  SU6656  |  Amodiaquine dihydrochloride dihydrate  |  Isobavachalcone  |  Ascomycin  |  Scutellarin  |  Mebendazole

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。