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Hu7691 free base

CAS No. : 2241232-43-7

MCE 站：Hu7691 free base

产品活性：Hu7691 free base 是一种具有口服活性的，选择性 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 的 IC₅₀ 分别为 4.0 nM、97.5 nM、28 nM。Hu7691 free base 抑制肿瘤生长并降低小鼠的皮肤毒性。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Protein Tyrosine Kinase/RTK  |  TGF-beta/Smad  |  Epigenetics  |  Cell Cycle/DNA Damage  |  Cytoskeleton  |  MAPK/ERK Pathway  |  Metabolic Enzyme/Protease

作用靶点：Akt  |  PKA  |  PKC  |  ROCK  |  Ribosomal S6 Kinase (RSK)  |  SGK

In Vitro: Hu7691 free base displays low inhibitions against most of the kinases in the four families (AGC, TK, TKL, Lipid/Atypical; PKA, IC₅₀=11 nM; PKCη, IC₅₀=629 nM; ROCK1, IC₅₀=354 nM; RSK1, IC₅₀=756 nM; P70S6K, IC₅₀=229 nM; SGK, IC₅₀=1009 nM).
Hu7691 free base (2.25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473).
Hu7691 free base (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC₅₀ value of 15.2 μM.
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 IC₅₀ range of 0.6-27 μM. Hu7691 free base shows low antiproliferation activities against the HL7702 ａnd HPDE6-C7 normal cells, exhibiting IC₅₀ values of 5.4 ａnd 16.1 μM, respectively.

In Vivo: Hu7691 free base (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition.
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.
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.
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).

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