2. PI3K/Akt/mTOR TGF-beta/Smad Stem Cell/Wnt Epigenetics Cytoskeleton Cell Cycle/DNA Damage MAPK/ERK Pathway Metabolic Enzyme/Protease
  3. Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK
  4. 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。

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Hu7691 free base Chemical Structure

Hu7691 free base Chemical Structure

CAS No. : 2241232-43-7

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Customer Review

Other Forms of Hu7691 free base:

Hu7691 free base 相关抗体

Top Publications Citing Use of Products

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 PKC 亚型特异性产品:

查看所有亚型
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

查看 ROCK 亚型特异性产品:

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ROCK ROCK1 ROCK2

查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

查看所有亚型
p70S6K RSK1 RSK2 RSK3 RSK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Hu7691 free base 相关抗体:

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].

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.
分子量

414.42

Formula

C22H21F3N4O
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.
纯度 & 产品资料
参考文献

Hu7691 free base 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hu76912241232-43-7Hu 7691Hu-7691AktPKAPKCROCKRibosomal S6 Kinase (RSK)SGKPKBProtein kinase BProtein kinase AProtein kinase CRho-associated protein kinaseRho-associated kinaseRho-kinaseROKS6KSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseorallycutaneoustoxicityAGCTKTKLLipid/AtypicalS473U87-MGU251A549HepG2HT-29KHOSMDA-MB-231PC3SKOV3Inhibitorinhibitorinhibit

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