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124033 Akt Inhibitor XVI, AT7867 - Calbiochem

124033
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₀H₂₀ClN₃

Products

Catalogue NumberPackaging Qty/Pack
124033-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced potency toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM). Shown to reduce cellular phosphorylation of GSK-3β (IC50 range from 2.08 to 4.45 µM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC50 range from 0.94 to 11.86 µM) and in mice in vivo (20 mg/kg via i.p. or 90 mg/kg via p.o.).
Catalogue Number124033
Brand Family Calbiochem®
Synonymsp70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
References
ReferencesGrimshaw, K.M., et al. 2010. Mol. Cancer Ther. 9, 1100.
Saxty, G., et al. 2007. J. Med. Chem. 50, 2293.
Product Information
FormWhite powder
Hill FormulaC₂₀H₂₀ClN₃
Chemical formulaC₂₀H₂₀ClN₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥99% 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
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Akt Inhibitor XVI, AT7867 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Akt Inhibitor XVI, AT7867 - Calbiochem Certificates of Analysis

TitleLot Number
124033

References

Reference overview
Grimshaw, K.M., et al. 2010. Mol. Cancer Ther. 9, 1100.
Saxty, G., et al. 2007. J. Med. Chem. 50, 2293.
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.

Revision23-May-2013 JSW
Synonymsp70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
DescriptionA cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced activity toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM), including PDK1, PI 3-Kβ, SGK, GSK-3β, and MEK1. Shown to effectively reduce the phosphorylation levels of GSK-3β, S6R, and FKHRL1 (IC50 range from 2.08 to 4.45 µM against GSK-3β pSer9 level), as well as inhibit the proliferation (IC50 range from 0.94 to 11.86 µM) of cancer cells exhibiting constitutive Akt pathway activation, including the PTEN-deficient MES-SA uterine sarcoma and U87MG glioblastoma cell lines. AT7867 treatments via i.p. or p.o. (20 mg/kg and 90 mg/kg, respectively, once every 3 days) are also reported to result in Akt pathway and tumor growth inhibition in mice bearing MES-SA (~40% of untreated control on day 10 by i.p. or p.o.) or U87MG (~50% of untreated control on day 10 by i.p.) xenograft in vivo.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₀H₂₀ClN₃
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (100 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesGrimshaw, K.M., et al. 2010. Mol. Cancer Ther. 9, 1100.
Saxty, G., et al. 2007. J. Med. Chem. 50, 2293.