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Hu7691 free base
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Hu7691 free base图片
CAS NO:2241232-43-7
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Hu7691 free base 是一种具有口服活性的，选择性Akt抑制剂，对 Akt1、Akt2 和 Akt3 的IC50分别为 4.0 nM、97.5 nM、28 nM。Hu7691 free base 抑制肿瘤生长并降低小鼠的皮肤毒性。
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)

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).
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.
分子量

414.42

Formula

C22H21F3N4O

CAS 号

2241232-43-7

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.