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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2241232-43-7
- 分子式: C22H21F3N4O
- 分子量:414.42
-
保管条件:
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]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
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) |
体外実験
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).
体内実験
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.
化学情報
-
CAS 番号 2241232-43-7
-
分子量 414.42
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Hu7691 free base 関連分類
HY-132302A 関連分類
Powered by Bioz