上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Hu7691 free base
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。
Hu7691 free base Chemical Structure
CAS No. : 2241232-43-7
| 规格 |
|
是否有货 |
|
| 100 mg |
|
询价 |
|
| 250 mg |
|
询价 |
|
| 500 mg |
|
询价 |
|
* Please select Quantity before adding items.
| 生物活性 |
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[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 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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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 T1/2 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].
Shanghai Jinpan Biotech Co Ltd 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. |
|
| 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.
|
| 参考文献 |
-
[1]. Jinxin Che, et al. Discovery of N-((3 S,4 S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1 H-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity. J Med Chem. 2021 Aug 26;64(16):12163-12180.
|
所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务
