1. PI3K/Akt/mTOR
  2. Akt

AKT-IN-1 

Cat. No.: HY-18296 Purity: 99.22%
Handling Instructions

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.

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

AKT-IN-1 Chemical Structure

AKT-IN-1 Chemical Structure

CAS No. : 1357158-81-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 363 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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View All Akt Isoform Specific Products:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.

IC50 & Target

IC50: 1.042 μM (AKT)[1]

In Vitro

AKT-IN-1 (Compound 26) is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40[1].

In Vivo

The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition[1].

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (72.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9119 mL 14.5594 mL 29.1189 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

343.42

Formula

C₂₂H₂₁N₃O

CAS No.

1357158-81-6

SMILES

NC(C1=CN=C(C2=CC=C(C3(N)CCC3)C=C2)C(C4=CC=CC=C4)=C1)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AKT-IN-1
Cat. No.:
HY-18296
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AKT-IN-1

Cat. No.: HY-18296