1. 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
  2. Akt
    PKA
    PKC
    ROCK
    Ribosomal S6 Kinase (RSK)
    SGK
  3. Hu7691

Hu7691 

Cat. No.: HY-132302
Handling Instructions

Hu7691 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 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.

For research use only. We do not sell to patients.

Hu7691 Chemical Structure

Hu7691 Chemical Structure

CAS No. : 2360523-76-6

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Description

Hu7691 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 inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].

IC50 & Target[1]

Akt1

4.0 nM (IC50)

Akt2

97.5 nM (IC50)

Akt3

28 nM (IC50)

PKA

11 nM (IC50)

PKCη

629 nM (IC50)

ROCK1

354 nM (IC50)

RSK1

756 nM (IC50)

p70S6K

229 nM (IC50)

In Vitro

Hu7691 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 (2.25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473)[1].
B5 (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC50 value of 15.2 μM[1].
Hu7691 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 shows low antiproliferation activities against the HL7702 and HPDE6-C7 normal cells, exhibiting IC50 values of 5.4 and 16.1 μM, respectively[1].

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

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).
In Vivo

Hu7691 (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition[1].
Hu7691 (15 mg/kg; oral) has a T1/2 of 8.68 hours, a Cmax of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h in rats[1].
Hu7691 (2 mg/kg; iv) has a T1/2 of 6.24 hours, a Cmax of 207.52 ng/mL and an AUC of 532.87 ng/mL•h in rats[1].
Hu7691 (20 mg/kg; oral) has a T1/2 of 16.7 hours, a Cmax of 905.65 ng/mL and an AUC of 36303 ng/mL•h in beagle dog (male, 40 weeks old, 8–10 kg)[1].

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

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 T1/2 of 8.68 hours, a Cmax of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h.
Molecular Weight

450.88

Formula

C₂₂H₂₂ClF₃N₄O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Hu7691
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