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528121 PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem

The PI 3-K/PDK-1 Inhibitor, NVP-BAG956, also referenced under CAS 853910-02-8, controls the biological activity of PI 3-K/PDK-1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: α,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile , BAG956, PDK1 Inhibitor IV, PI 3-K Inhibitor XVI

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528121
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
853910-02-8C₂₈H₂₁N₅

Products

Catalog NumberPackaging Qty/Pack
528121-5MG Glass bottle 5 mg
Description
OverviewA cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC50 >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).
Catalogue Number528121
Brand Family Calbiochem®
Synonymsα,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile , BAG956, PDK1 Inhibitor IV, PI 3-K Inhibitor XVI
References
ReferencesMarone, R., et al. 2009. Mol. Cancer Res. 7, 601.
Weisberg, E., et al. 2008. Blood 111, 3723.
Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.
Product Information
CAS number853910-02-8
FormOrange powder
Hill FormulaC₂₈H₂₁N₅
Chemical formulaC₂₈H₂₁N₅
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% 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 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem Certificates of Analysis

TitleLot Number
528121

References

Reference overview
Marone, R., et al. 2009. Mol. Cancer Res. 7, 601.
Weisberg, E., et al. 2008. Blood 111, 3723.
Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.
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.

Revision21-October-2011 RFH
Synonymsα,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile , BAG956, PDK1 Inhibitor IV, PI 3-K Inhibitor XVI
DescriptionA cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC50 >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).
FormOrange powder
Intert gas (Yes/No) Packaged under inert gas
CAS number853910-02-8
Chemical formulaC₂₈H₂₁N₅
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
+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
ReferencesMarone, R., et al. 2009. Mol. Cancer Res. 7, 601.
Weisberg, E., et al. 2008. Blood 111, 3723.
Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.