Hu7691 free base 

Hu7691 free base is an orally active, selective Akt inhibitor with IC₅₀s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice^[1].

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)^[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 IC₅₀ 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 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

414.42

C₂₂H₂₁F₃N₄O

2241232-43-7

O=C(N[C@@H]1CNCC[C@H]1C2=CC=C(F)C(F)=C2)C3=CC=C(C4=CC=NN4C)C=C3F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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):1  [Content Brief]