貨號	規(guī)格	價(jià)格	上海	北京	武漢	南京
S82808-1mg	99.5%	￥442.00 S82808-1mg ￥442.00 現(xiàn)貨	10 10	-	-	-
S82808-5mg	99.5%	￥625.60 S82808-5mg ￥625.60 現(xiàn)貨	8 8	-	-	-
S82808-10mg	99.5%	￥1190.00 S82808-10mg ￥1190.00 現(xiàn)貨	4 4	-	-	-
S82808-50mg	99.5%	￥4600.00 S82808-50mg ￥4600.00 現(xiàn)貨	2 2	-	-	-
S82808-100mg	≥98%	￥7300.00 S82808-100mg ￥7300.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania

產(chǎn)品描述：

靶點(diǎn)：

Akt1:2.7 nM (IC50);Leishmania;Akt3:8.1 nM (IC50);Akt2:14 nM (IC50);Akt1 E17K mutant;Akt;?Parasite

體外研究：

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

體內(nèi)研究：

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

參考文獻(xiàn)：

1. Lapierre JM, 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 Inhibitor. J Med Chem. 2016 Jul 14;59(13):6455-69. 2. Devki Nandan, et al. Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania. PLoS One. 2018 Nov 6;13(11):e0206920.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.312 ml	11.56 ml	23.12 ml
5 mM	0.462 ml	2.312 ml	4.624 ml
10 mM	0.231 ml	1.156 ml	2.312 ml
50 mM	0.046 ml	0.231 ml	0.462 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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