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Akt1 and Akt2-IN-1

Catalog No. T14152 CAS 893422-47-4

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM). It has potent and balanced activity.

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Akt1 and Akt2-IN-1, CAS 893422-47-4

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 347.00
25 mg	6-8 weeks	$ 1,140.00
50 mg	6-8 weeks	$ 1,490.00
100 mg	6-8 weeks	$ 1,990.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 413.00

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Biological Description

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Description	Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM). It has potent and balanced activity.
Targets&IC50	Akt2:42 nM, Akt1:3.5 nM
In vitro	Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein[1]. Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition. Akt1 and Akt2-IN-1 (Compound 17) 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).
In vivo	Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1 and Akt2-IN-1 (Compound 17) 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 and Akt2-IN-1 (Compound 17), tolerability and Akt inhibition are assessed in mice. Akt1 and Akt2-IN-1 (Compound 17) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy and has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung[1].

Molecular Weight	539.63
Formula	C33H29N7O
CAS No.	893422-47-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35 mg/mL (64.86 mM)

References and Literature

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.

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Keywords

Akt1 and Akt2-IN-1 893422-47-4 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt Akt-1 and Akt2-IN-1 Akt1 and Akt2IN1 Akt1 and Akt2 IN 1 inhibitor inhibit

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