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260962 DNA-PK Inhibitor III - CAS 404009-40-1 - Calbiochem

260962
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₂H₁₅NO₃404009-40-1

Products

Catalogue NumberPackaging Qty/Pack
260962-1MG Plastic ampoule 1 mg
Description
OverviewA cell-permeable aryl-morpholino compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 120 nM) and PI 3-Kinase catalytic subunit p110β (IC50 = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 µM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI 3-K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4, 0.88, and 1.0 µM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM.
Catalogue Number260962
Brand Family Calbiochem®
SynonymsIC86621, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
References
ReferencesKashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257.
Willmore, E., et al. 2004. Blood,103, 4659.
Product Information
CAS number404009-40-1
ATP CompetitiveY
FormOff-white solid
Hill FormulaC₁₂H₁₅NO₃
Chemical formulaC₁₂H₁₅NO₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetDNA-PK
Primary Target IC<sub>50</sub>120 nM against DNA-PK
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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 Carcinogenic / Teratogenic
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

DNA-PK Inhibitor III - CAS 404009-40-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

DNA-PK Inhibitor III - CAS 404009-40-1 - Calbiochem Certificates of Analysis

TitleLot Number
260962

References

Reference overview
Kashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257.
Willmore, E., et al. 2004. Blood,103, 4659.
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.

Revision04-January-2010 RFH
SynonymsIC86621, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
DescriptionA cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 0.12 µM) and the PI-3 kinase catalytic subunit p110β (IC50 = 0.135 µM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 µM) and enhances DSB-induced anti-tumor activity both in vitro and in vivo. Exhibits no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI3K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4 µM, 880 nM, and 1 µM, respectively) and does not inhibit a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number404009-40-1
Chemical formulaC₁₂H₁₅NO₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (5 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 Carcinogenic / Teratogenic
ReferencesKashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257.
Willmore, E., et al. 2004. Blood,103, 4659.