Akt1 and Akt2-IN-1

Modify Date: 2024-01-13 20:55:05

Akt1 and Akt2-IN-1 structure	Common Name	Akt1 and Akt2-IN-1
	CAS Number	893422-47-4	Molecular Weight	539.63000
	Density	1.3±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₃₃H₂₉N₇O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Akt1 and Akt2-IN-1

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

Name	3-Phenyl-2-[4-({4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl}methyl)phenyl]-1,6-naphthyridin-5(6H)-one
Synonym	More Synonyms

Description	Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
Related Catalog	Research Areas >> Cancer
Target	Akt1:3.5 nM (IC50) Akt2:42 nM (IC50)
In Vitro	Consistent with the allosteric mode of inhibition, Akt1 and 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 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].
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) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. 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. 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].
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.

Density	1.3±0.1 g/cm3
Molecular Formula	C₃₃H₂₉N₇O
Molecular Weight	539.63000
Exact Mass	539.24300
PSA	103.45000
LogP	3.59
Index of Refraction	1.666
Storage condition	2-8℃

1,6-Naphthyridin-5(6H)-one, 3-phenyl-2-[4-[[4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl]methyl]phenyl]-

3-Phenyl-2-[4-({4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl}methyl)phenyl]-1,6-naphthyridin-5(6H)-one

Akt1 and Akt2-IN-1

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Akt1 and Akt2-IN-1
Price: Negotiable
Purity: 99.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: Akt1 and Akt2-IN-1
Price: $750.0/100mg $1350.0/250mg $2700.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: Akt1 and Akt2-IN-1
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: ALLOSTERIC INHIBITORS OF AKT 1
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Delivery: Inquiry
Contact: Ms Wang
Email: enquiry@dycnchem.com

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Price: $499/10mM*1mLinDMSO

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