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528100 PI-103 - CAS 371935-74-9 - Calbiochem

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.

PI-103 - CAS 371935-74-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V

Primary Target: DNA-PK, PI3-K, and mTOR
528100
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
371935-74-9C₁₉H₁₆N₄O₃

Products

Catalogue NumberPackaging Qty/Pack
528100-1MG Plastic ampoule 1 mg
528100-5MG Plastic ampoule 5 mg
Description
OverviewA cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC50 = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC50 = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo. A 10 mM (2 mg/574 µl) solution of PI-103 (Cat. No. 528101) in DMSO is also available.
Catalogue Number528100
Brand Family Calbiochem®
Synonyms3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V
References
ReferencesRaynaud, F.I., et al. 2007. Cancer Res. 67, 5840.
Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
Knight, Z.A., et al. 2006. Cell 125, 733.
Product Information
CAS number371935-74-9
ATP CompetitiveY
FormWhite solid
Hill FormulaC₁₉H₁₆N₄O₃
Chemical formulaC₁₉H₁₆N₄O₃
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetDNA-PK, PI3-K, and mTOR
Primary Target IC<sub>50</sub>2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110delta;, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively
Purity≥97% 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 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
528100-1MG 04055977270457
528100-5MG 04055977270464

Documentation

PI-103 - CAS 371935-74-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PI-103 - CAS 371935-74-9 - Calbiochem Certificates of Analysis

TitleLot Number
528100

References

Reference overview
Raynaud, F.I., et al. 2007. Cancer Res. 67, 5840.
Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
Knight, Z.A., et al. 2006. Cell 125, 733.

Posters

Title
Human Kinome & InhibitorSelect™ Libraries
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.

Revision13-October-2010 RFH
Synonyms3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V
DescriptionA cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC50 = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC50 = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number371935-74-9
Chemical formulaC₁₉H₁₆N₄O₃
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (5 mg/ml). Slight warming may be required for complete solubilization.
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
ReferencesRaynaud, F.I., et al. 2007. Cancer Res. 67, 5840.
Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
Knight, Z.A., et al. 2006. Cell 125, 733.