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521276 PDK1 Inhibitor II - CAS 850717-64-5 - Calbiochem

The PDK1 Inhibitor II, also referenced under CAS 850717-64-5, controls the biological activity of PDK1. 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: 2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517

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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
850717-64-5C₁₅H₁₄N₄O₂

Products

Catalog NumberPackaging Qty/Pack
521276-5MG 5 mg
Description
OverviewA cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM) and effectively suppresses cellular Akt Thr308 phosphorylation level in PC-3 cultures (IC50 ≤1 µM), while affecting PKA (IC50 = 1.6 µM) and 7 other kinases (IC50 ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 µg/ml in PBS) and poor pharmacokinetics.
Catalogue Number521276
Brand Family Calbiochem®
Synonyms2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517
References
ReferencesIslam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3819.
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3814.
Product Information
CAS number850717-64-5
FormDark brown solid
Hill FormulaC₁₅H₁₄N₄O₂
Chemical formulaC₁₅H₁₄N₄O₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC (sum of two isomers)
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
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

PDK1 Inhibitor II - CAS 850717-64-5 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PDK1 Inhibitor II - CAS 850717-64-5 - Calbiochem Certificates of Analysis

TitleLot Number
521276

References

Reference overview
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3819.
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3814.
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.

Revision18-April-2011 RFH
Synonyms2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517
DescriptionA cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM) and effectively suppresses cellular Akt Thr308 phosphorylation level in PC-3 cultures (IC50 ≤1 µM), while affecting PKA (IC50 = 1.6 µM) and 7 other kinases (IC50 ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 µg/ml in PBS) and poor pharmacokinetics.
FormDark brown solid
Intert gas (Yes/No) Packaged under inert gas
CAS number850717-64-5
Chemical formulaC₁₅H₁₄N₄O₂
Structure formulaStructure formula
Purity≥95% by HPLC (sum of two isomers)
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 3 months at -20°C.
Toxicity Standard Handling
ReferencesIslam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3819.
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3814.