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.
For research use only. We do not sell to patients.
- CAS No.: 2241232-43-7
- Formula: C22H21F3N4O
- Molecular Weight:414.42
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
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) |
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.
-
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).
Hu7691 free base (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 free base (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 free base (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].
MedChemExpress (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.
Chemical Information
-
CAS No. 2241232-43-7
-
Molecular Weight 414.42
-
Formula C22H21F3N4O
-
SMILES
O=C(N[C@@H]1CNCC[C@H]1C2=CC=C(F)C(F)=C2)C3=CC=C(C4=CC=NN4C)C=C3F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hu7691 free base Related Classifications
HY-132302A Related Classifications
Powered by Bioz