產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 50mg 100mg
CAS	1313881-70-7
別名	N/A
化學(xué)名	N/A
分子式	C27H24N6
分子量	432.52
溶解度	DMSO : ≥ 40.2 mg/mL (92.94 mM)
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

ARQ-092 is an orally bioavailable, selective, and potent allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.

ARQ-092 (Compound 21a) demonstrates high enzymatic potency against Akt1, Akt2 and Akt3, as well as potent cellular inhibition of Akt activation and the phosphorylation of the downstream target PRAS40. ARQ-092 shows strong affinity for un-phosphorylated fulllength Akt1 and potently inhibited the phosphorylated form of full-length Akt isoforms. In a large panel of cell lines derived from various tumor types, ARQ-092 shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. ARQ-092 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 ARQ-092 (IC50=0.31 uM)[1].

In a mouse pharmacokinetic study, (po at 100 mg/kg, iv at 5 mg/kg), ARQ-092 (Compound 21a) shows an oral bioavailability of 23%. ARQ-092 results in 99%, 95% and 58% reductions in p-Akt (S473), p-Akt (T306) and p-PRAS40 (T246), respectively, after tumor-bearing mice are treated with 100 mg/kg po. The inhibition of phosphorylation is sustained at eight hours.The plasma concentration of ARQ-092 at one hour is 2.1 uM and decreased to 0.26 uM at 8 hours, while in the tumor, the concentration is 21.0 uM at one hour and 9.6 uM at 8 hours[1]. To determine the effects of ARQ-092 on cardiac function, echocardiographic analysis of SHP2+/+ and SHP2Y279C/+ littermates is conducted, either in the presence of orally administered vehicle or ARQ-092 (100 mg/kg/day), at 12, 14, and 16 weeks of age. By 12 weeks of age, SHP2Y279C/+ mice show significant left ventricular hypertrophy, as indicated by decreased chamber dimension and increased posterior wall thickness compared with those of littermate controls; hypertrophy in these mice continued to progress over the 4 week time period. Treatment of the SHP2Y279C/+ mice with ARQ-092 normalizes the hypertrophic cardiomyopathy (HCM) phenotype as early as 2 weeks following treatment, with levels comparable to those in SHP2+/+ at this time point[2].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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