| 生物活性 | Hu7691 is an orally active, selectiveAktinhibitor withIC50s of 4.0 nM, 97.5 nM, 28 nM forAkt1,Akt2andAkt3, 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) |
|
体外研究
(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 IC50value 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 IC50range of 0.6-27 μM. Hu7691 shows low antiproliferation activities against the HL7702 and HPDE6-C7 normal cells, exhibiting IC50values of 5.4 and 16.1 μM, respectively[1].
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). |
|
体内研究
(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 T1/2of 8.68 hours, a Cmaxof 171.17 ng/mL and an AUC of 2820.64 ng/mLoh in rats[1].
Hu7691 (2 mg/kg; iv) has a T1/2of 6.24 hours, a Cmaxof 207.52 ng/mL and an AUC of 532.87 ng/mLoh in rats[1].
Hu7691 (20 mg/kg; oral) has a T1/2of 16.7 hours, a Cmaxof 905.65 ng/mL and an AUC of 36303 ng/mLoh in beagle dog (male, 40 weeks old, 8–10 kg)[1].
| 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 T1/2of 8.68 hours, a Cmaxof 171.17 ng/mL and an AUC of 2820.64 ng/mLoh. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com