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539652 PKCβII/EGFR Inhibitor - CAS 145915-60-2 - Calbiochem

539652
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
145915-60-2C₂₀H₁₃F₂N₃O₂
Description
OverviewA cell-permeable symmetrical phthalimide compound that acts as a potent, reversible, and ATP-competitive inhibitor of EGFR and PKC isozymes α, βI, and βII (IC50 = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.
Catalogue Number539652
Brand Family Calbiochem®
SynonymsCG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
References
ReferencesKouroedov, A., et al. 2004. Circulation 110, 91.
Lee, S.W., et al. 2003. Bone 32, 217.
Perrotti, D., et al. 1998. EMBO J. 17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol. 10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res. 1, 813.
Trinks, U., et al. 1994. J. Med. Chem. 37, 1015.
Product Information
CAS number145915-60-2
ATP CompetitiveY
FormOrange solid
Hill FormulaC₂₀H₁₃F₂N₃O₂
Chemical formulaC₂₀H₁₃F₂N₃O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetEGFR
Primary Target IC<sub>50</sub>0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM against EGFR and PKC isozymes α, βI, and βII, respectively
Purity≥98% 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 +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
Global Trade Item Number
Catalogue Number GTIN
539652 0

Documentation

PKCβII/EGFR Inhibitor - CAS 145915-60-2 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

PKCβII/EGFR Inhibitor - CAS 145915-60-2 - Calbiochem Certificates of Analysis

TitleLot Number
539652

References

Reference overview
Kouroedov, A., et al. 2004. Circulation 110, 91.
Lee, S.W., et al. 2003. Bone 32, 217.
Perrotti, D., et al. 1998. EMBO J. 17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol. 10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res. 1, 813.
Trinks, U., et al. 1994. J. Med. Chem. 37, 1015.
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.

Revision11-January-2010 RFH
SynonymsCG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
DescriptionA cell-permeable, potent, ATP-competitive, and reversible inhibitor of EGFR and PKC isozymes α, βI, and βII (IC50 = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.
FormOrange solid
Intert gas (Yes/No) Packaged under inert gas
CAS number145915-60-2
Chemical formulaC₂₀H₁₃F₂N₃O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (20 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
ReferencesKouroedov, A., et al. 2004. Circulation 110, 91.
Lee, S.W., et al. 2003. Bone 32, 217.
Perrotti, D., et al. 1998. EMBO J. 17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol. 10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res. 1, 813.
Trinks, U., et al. 1994. J. Med. Chem. 37, 1015.