1. PI3K/Akt/mTOR
  2. Akt
  3. Akt1/Akt2-IN-1

Akt1/Akt2-IN-1 (Compound 17) 是一种有效的变构抑制剂,抑制 Akt1 (IC50=3.5 nM) 和 Akt2 (IC50=42 nM)。

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Akt1/Akt2-IN-1 Chemical Structure

Akt1/Akt2-IN-1 Chemical Structure

CAS No. : 893422-47-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3324
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1 mg ¥1590
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5 mg ¥2800
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10 mg ¥4200
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Customer Review

查看 Akt 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity[1].

IC50 & Target[1]

Akt1

3.5 nM (IC50)

Akt2

42 nM (IC50)

体外研究
(In Vitro)

Consistent with the allosteric mode of inhibition, Akt1/Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC50=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1/Akt2-IN-1 has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein[1].

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

体内研究
(In Vivo)

Akt1/Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1/Akt2-IN-1 has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1/Akt2-IN-1 has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1/Akt2-IN-1 shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1/Akt2-IN-1, tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1/Akt2-IN-1 is well tolerated in mice and shows high levels of Akt inhibition in mouse lung[1].

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

分子量

539.63

Formula

C33H29N7O

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 35 mg/mL (64.86 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8531 mL 9.2656 mL 18.5312 mL
5 mM 0.3706 mL 1.8531 mL 3.7062 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Akt1/Akt2-IN-1 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8531 mL 9.2656 mL 18.5312 mL 46.3280 mL
5 mM 0.3706 mL 1.8531 mL 3.7062 mL 9.2656 mL
10 mM 0.1853 mL 0.9266 mL 1.8531 mL 4.6328 mL
15 mM 0.1235 mL 0.6177 mL 1.2354 mL 3.0885 mL
20 mM 0.0927 mL 0.4633 mL 0.9266 mL 2.3164 mL
25 mM 0.0741 mL 0.3706 mL 0.7412 mL 1.8531 mL
30 mM 0.0618 mL 0.3089 mL 0.6177 mL 1.5443 mL
40 mM 0.0463 mL 0.2316 mL 0.4633 mL 1.1582 mL
50 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9266 mL
60 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7721 mL
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.

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产品名称:
Akt1/Akt2-IN-1
目录号:
HY-50862
需求量: