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Hu7691 free base

产品编号 T39733 CAS 2241232-43-7

Hu7691 free base is an orally active, selective Akt inhibitor. It exhibits IC50 values of 4.0 nM, 97.5 nM, and 28 nM for Akt1, Akt2, and Akt3, respectively. Furthermore, it effectively inhibits tumor growth and facilitates a reduction in cutaneous toxicity in mice.

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Hu7691 free base, CAS 2241232-43-7

规格	价格/CNY	货期
1 mg	￥ 1,980	现货
5 mg	￥ 4,920	现货
10 mg	￥ 7,130	现货
25 mg	￥ 10,600	现货
50 mg	￥ 13,800	现货

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其他形式的 Hu7691 free base:

Hu7691
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纯度: 98.89% ee: 97.96%

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存储 & 溶解度

参考文献

产品描述	Hu7691 free base is an orally active, selective Akt inhibitor. It exhibits IC50 values of 4.0 nM, 97.5 nM, and 28 nM for Akt1, Akt2, and Akt3, respectively. Furthermore, it effectively inhibits tumor growth and facilitates a reduction in cutaneous toxicity in mice.
靶点活性	PKCη:629 nM (IC50), Akt3:28 nM (IC50), ROCK1:354 nM (IC50), p70 S6K:229 nM (IC50), PKA:11 nM (IC50), Akt2:97.5 nM (IC50), Akt1:4.0 nM (IC50), RSK1:756 nM (IC50)
体外活性	Hu7691 free base displays low inhibitions against most of the kinases in the four families (AGC, TK, TKL, Lipid/Atypical; PKA, IC 50 =11 nM; PKCη, IC 50 =629 nM; ROCK1, IC 50 =354 nM; RSK1, IC 50 =756 nM; P70S6K, IC 50 =229 nM; SGK, IC 50 =1009 nM)[1]. Hu7691 free base (2.25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473)[1]. Hu7691 free base (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC 50 value of 15.2 μM[1]. Hu7691 free base has a significant inhibitory effect on the growth of 18 kinds of human tumor cells (U87-MG, U251, A549, HepG2, HT-29, KHOS, MDA-MB-231, PC3, SKOV3 and so on) derived from different tissues, with the IC 50 range of 0.6-27 μM. Hu7691 free base shows low antiproliferation activities against the HL7702 and HPDE6-C7 normal cells, exhibiting IC 50 values of 5.4 and 16.1 μM, respectively[1]. Western Blot Analysis[1]Cell Line: HaCaT cells Concentration: 2.25, 4.5, 9, 18, 36 μM Incubation Time: 24 hours Result: Induced effective decrease of the phosphorylation level of Akt (S473).
体内活性	Hu7691 free base (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition[1]. Hu7691 free base (15 mg/kg; oral) has a T 1/2 of 8.68 hours, a C max of 171.17 ng/mL and an AUC of 2820.64 ng/mL?h in rats[1]. Hu7691 free base (2 mg/kg; iv) has a T 1/2 of 6.24 hours, a C max of 207.52 ng/mL and an AUC of 532.87 ng/mL?h in rats[1]. Hu7691 free base (20 mg/kg; oral) has a T 1/2 of 16.7 hours, a C max of 905.65 ng/mL and an AUC of 36303 ng/mL?h in beagle dog (male, 40 weeks old, 8–10 kg)[1]. Animal Model: Balb/c mice (nu/nu, female, 3-4 weeks old, 20-25 g) with 786-O and KHOS xenograft[1]Dosage: 12.5, 25, 50 mg/kg Administration: Oral; once daily for 22 days Result: Showed dose-dependent tumor growth inhibition. Animal Model: SD rats (male, 8 weeks old, 250-300 g)[1]Dosage: 15 mg/kg (Pharmacokinetic Analysis) Administration: Oral Result: Had a T 1/2 of 8.68 hours, a C max of 171.17 ng/mL and an AUC of 2820.64 ng/mL?h.

分子量	414.432
分子式	C22H21F3N4O
CAS No.	2241232-43-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Jinxin Che, et al. Discovery of N-((3 S,4 S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1 H-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity. J Med Chem. 2021 Aug 26;64(16):12163-12180.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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