| 生物活性 | Hu7691 free base is an orally active, selectiveAktinhibitor withIC50s of 4.0 nM, 97.5 nM, 28 nM forAkt1,Akt2andAkt3, respectively. Hu7691 free base 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) |
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体外研究
(In Vitro) | 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 IC50value 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 IC50range of 0.6-27 μM. Hu7691 free base 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). |
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体内研究
(In Vivo) | 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 T1/2of 8.68 hours, a Cmaxof 171.17 ng/mL and an AUC of 2820.64 ng/mLoh in rats[1].
Hu7691 free base (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 free base (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. |
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| 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. |
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