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

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.

For research use only. We do not sell to patients.

Akt1/Akt2-IN-1 Chemical Structure

Akt1/Akt2-IN-1 Chemical Structure

CAS No. : 893422-47-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 332 In-stock
Solution
10 mM * 1 mL in DMSO USD 332 In-stock
Solid
5 mg USD 280 In-stock
10 mg USD 420 In-stock
50 mg USD 1134 In-stock
100 mg USD 1700 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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)

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].

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

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].

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

Molecular Weight

539.63

Formula

C33H29N7O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC=C1)C2=C1N=C(C(C3=CC=CC=C3)=C2)C(C=C4)=CC=C4CN5CCC(CC5)C6=NNC(C7=NC=CC=C7)=N6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (64.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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
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Akt1/Akt2-IN-1 Related Classifications

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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Product Name:
Akt1/Akt2-IN-1
Cat. No.:
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