Miransertib
Cat. No.:YN420263
产品名称: | Miransertib |
CAS No.: | 1313881-70-7 |
Chemical Name: | 3-[3-[4-(1-aminocyclobutyl)phenyl]-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl]-2-pyridinamine |
Synonyms: | ARQ-092 |
分子量: | 432.52 |
分子式: | C₂₇H₂₄N₆ |
SMILES: | NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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)。 |
IC50和靶点: | [{name:"Akt1:2.7 nM (IC50)'}, 'Leishmania', {'Akt3:8.1 nM (IC50)"},{name: "Akt2:14 nM (IC50)'}, 'Akt1 E17K mutant'] |
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Yu, Y., Savage, R.E., Eathiraj, S., et al.Targeting AKT1-E17K and the PI3K/AKT pathway with an allosteric AKT inhibitor, ARQ 092PLoS One10(10),e0140479(2015)
Lapierre, J.-M., Eathiraj, S., Vensel, D., et al.Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An orally bioavailable, selective, and potent allosteric AKT inhibitorJ. Med. Chem.59(13),6455-6469(2016)
Kim, K., Li, J., Barazia, A., et al.ARQ 092, an orally-available, selective AKT inhibitor, attenuates neutrophil-platelet interactions in sickle cell diseaseHaematologica102(2),246-259(2016)
Lindhurst, M.J., Yourick, M.R., Yu, Y., et al.Repression of AKT signaling by ARQ 092 in cells and tissues from patients with Proteus syndromeSci. Rep.5(17162),(2015)