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521232 PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem

521232
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
205254-94-0C₂₇H₂₇N₅O₄
Description
Overview

This product has been discontinued.



A cell-permeable piperazinyl-quinazoline carboxamide compound that acts as a potent, ATP-competitive, reversible, and selective inhibitor of PDGF receptor family of tyrosine kinases (IC50 = 0.05 µM for α-PDGFR; 0.08 µM for β-PDGFR; 0.05 µM for c-Kit; 0.23 µM for Flt3). Affects the activities of other kinases only at much higher concentrations (IC50 ≥ 30 µM for EGFR, FGFR, Src, PKA & PKC). Reported to block the PDGF-BB induced proliferation of porcine aorta smooth muscle cells (IC50 = 0.25 µM).

Catalogue Number521232
Brand Family Calbiochem®
Synonyms4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide
References
ReferencesMatsuno, K., et al. 2003. J. Med. Chem. 46, 4910.
Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3001.
Matsuno, K., et al. 2002. J. Med. Chem. 45, 4513.
Matsuno, K., et al. 2002. J. Med. Chem. 45, 3057.
Product Information
CAS number205254-94-0
ATP CompetitiveY
FormWhite solid
Hill FormulaC₂₇H₂₇N₅O₄
Chemical formulaC₂₇H₂₇N₅O₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Targetα-PDGFR
Primary Target IC<sub>50</sub>0.05 µM for α-PDGFR; 0.08 µM for β-PDGFR; 0.05 µM for c-Kit; 0.23 µM for Flt3
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 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
Global Trade Item Number
Catalogue Number GTIN
521232 0

Documentation

PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem Certificates of Analysis

TitleLot Number
521232

References

Reference overview
Matsuno, K., et al. 2003. J. Med. Chem. 46, 4910.
Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3001.
Matsuno, K., et al. 2002. J. Med. Chem. 45, 4513.
Matsuno, K., et al. 2002. J. Med. Chem. 45, 3057.
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.

Revision12-January-2010 RFH
Synonyms4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide
DescriptionA cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of PDGF receptor family of tyrosine kinases (IC50 = 50 nM for α-PDGFR, 80 nM for β-PDGFR, 50 nM for c-Kit, and 230 nM for Flt3). Inhibits the activities of other kinases only at much higher concentrations (IC50 > 30 µM for EGFR, FGFR, Src, PKA, and PKC). Reported to block PDGF-BB-induced proliferation of porcine aorta smooth muscle cells (IC50 = 250 nM).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number205254-94-0
Chemical formulaC₂₇H₂₇N₅O₄
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 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 Carcinogenic / Teratogenic
ReferencesMatsuno, K., et al. 2003. J. Med. Chem. 46, 4910.
Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3001.
Matsuno, K., et al. 2002. J. Med. Chem. 45, 4513.
Matsuno, K., et al. 2002. J. Med. Chem. 45, 3057.