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528117 PI 3-K inhibitor IX, PIK-90 - CAS 677338-12-4 - Calbiochem

The PI 3-K inhibitor IX, PIK-90, also referenced under CAS 677338-12-4, controls the biological activity of PI 3-K. 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: N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI

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528117
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
677338-12-4C₁₈H₁₇N₅O₃

Products

Catalogue NumberPackaging Qty/Pack
528117-5MGCN Plastic ampoule 5 mg
Description
OverviewA cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).
Catalogue Number528117
Brand Family Calbiochem®
SynonymsN-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI
References
ReferencesFan, Q.W., et al. 2007. Cancer Res. 67, 7960.
Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
Knight, Z.A., et al. 2006. Cell 125, 733.
Product Information
CAS number677338-12-4
FormPale yellow solid
Hill FormulaC₁₈H₁₇N₅O₃
Chemical formulaC₁₈H₁₇N₅O₃
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
S PhraseS: 22-24/25

Do not breathe dust.
Avoid contact with skin and eyes.
Product Usage Statements
Storage and Shipping Information
Ship Code Blue Ice Only
Toxicity Standard Handling
Storage -20°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
Global Trade Item Number
Catalogue Number GTIN
528117-5MGCN 04055977197006

Documentation

PI 3-K inhibitor IX, PIK-90 - CAS 677338-12-4 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PI 3-K inhibitor IX, PIK-90 - CAS 677338-12-4 - Calbiochem Certificates of Analysis

TitleLot Number
528117

References

Reference overview
Fan, Q.W., et al. 2007. Cancer Res. 67, 7960.
Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
Knight, Z.A., et al. 2006. Cell 125, 733.
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.

Revision10-February-2011 RFH
SynonymsN-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI
DescriptionA cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number677338-12-4
Chemical formulaC₁₈H₁₇N₅O₃
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (0.5 mg/ml). Slight warming may be required to for complete solubility.
Storage Protect from light
-20°C
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
ReferencesFan, Q.W., et al. 2007. Cancer Res. 67, 7960.
Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
Knight, Z.A., et al. 2006. Cell 125, 733.