Akt1/Akt2-IN-1

Name: Akt1/Akt2-IN-1
Brand: MedChemExpress
SKU: HY-50862
Rating: 4.5 (1 reviews)

Cat. No.: HY-50862 Purity: 99.30%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 332	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1134	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1700	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Akt Akt1 Akt2 Akt3

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References
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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)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	5610 nM Compound: 1	Inhibition of human ERG expressed in HEK cells by competitive radioligand binding assay Inhibition of human ERG expressed in HEK cells by competitive radioligand binding assay	[PMID: 19097777]

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.

893422-47-4

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
10 mM	0.1853 mL	0.9266 mL	1.8531 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.30%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (247 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Bilodeau MT, Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82. [Content Brief]

Complete Stock Solution Preparation Table

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

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.

Keywords:

Akt1/Akt2-IN-1893422-47-4AktPKBProtein kinase BInhibitorinhibitorinhibit

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Akt1/Akt2-IN-1

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Akt1/Akt2-IN-1 Related Antibodies

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Complete Stock Solution Preparation Table

Akt1/Akt2-IN-1 Related Classifications

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