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124034 Akt Inhibitor XV, Isozyme-Selective - Calbiochem

124034
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₃H₂₉N₇O

Products

Catalogue NumberPackaging Qty/Pack
124034-2MG Glass bottle 2 mg
Description
OverviewA cell-permeable naphthyridinone compound that acts as an allosteric Akt1/2-selective inhibitor (IC50 = 3.5, 42, and 1900 nM against Akt1, Akt2, and Akt3, respectively) in a PH domain-dependent, but not ATP-competitive, manner, with little activity against a panel of more than 160 other kinases, including the related AGC family kinases (inactive at 10 µM against GSK, PDK1, PKA, PKC, and SGK). Effectively inhibits the basal Akt phosphorylation in cancer cells with deregulated Akt pathway activation, including the HCT116 colorectal carcinoma and a panel of breast cancer cell lines (IC50 <500 nM), and suppresses Akt-dependent cell growth both in cultures in vitro (IC50 ≤1 µM) and in mice in vivo (50 to 100 mg/kg, SC). Although also referred to as AKTi-1/2, this is not the same compound as Akt Inhibitor XV (Cat. Nos. 124017 & 124018).
Catalogue Number124034
Brand Family Calbiochem®
Synonyms5-Hydroxy-3-phenyl-2-(4-((4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperdin-1-yl)methyl)phenyl)-1,6-naphthyridine
References
ReferencesShe, Q.B., et al. 2010. Cancer Cell 18, 39.
Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett. 18, 3178.
She, Q.B, et al. 2008. PLoS One 3, e3065.
Product Information
FormWhite powder
Hill FormulaC₃₃H₂₉N₇O
Chemical formulaC₃₃H₂₉N₇O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications

Documentation

Akt Inhibitor XV, Isozyme-Selective - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Akt Inhibitor XV, Isozyme-Selective - Calbiochem Certificates of Analysis

TitleLot Number
124034

References

Reference overview
She, Q.B., et al. 2010. Cancer Cell 18, 39.
Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett. 18, 3178.
She, Q.B, et al. 2008. PLoS One 3, e3065.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision02-November-2011 RFH
Synonyms5-Hydroxy-3-phenyl-2-(4-((4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperdin-1-yl)methyl)phenyl)-1,6-naphthyridine
DescriptionA cell-permeable naphthyridinone compound that acts as an allosteric Akt1/2-selective inhibitor (IC50 = 3.5, 42, and 1900 nM against Akt1, Akt2, and Akt3, respectively) in a PH domain-dependent, but not ATP-competitive, manner, with little activity against a panel of more than 160 other kinases, including the related AGC family kinases (inactive at 10 µM against GSK, PDK1, PKA, PKC, and SGK). Effectively inhibits the basal Akt phosphorylation in cancer cells with deregulated Akt pathway activation, including the HCT116 colorectal carcinoma and a panel of breast cancer cell lines (IC50 <500 nM), and suppresses Akt-dependent cell growth both in cultures in vitro (IC50 ≤1 µM) and in mice in vivo (50 to 100 mg/kg, SC). Although also referred to as AKTi-1/2, this is not the same compound as Akt Inhibitor XV (Cat. Nos. 124017 & 124018).
FormWhite powder
Chemical formulaC₃₃H₂₉N₇O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (25 mg/ml)
Storage +2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesShe, Q.B., et al. 2010. Cancer Cell 18, 39.
Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett. 18, 3178.
She, Q.B, et al. 2008. PLoS One 3, e3065.