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521231 PDGFR Tyrosine Kinase Inhibitor II - CAS 249762-74-1 - Calbiochem

The PDGFR Tyrosine Kinase Inhibitor II, also referenced under CAS 249762-74-1, controls the biological activity of PDGFR Tyrosine Kinase. 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: (5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476

Primary Target: PDGFR in swiss 3T3 cells
521231
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
249762-74-1C₂₁H₁₈N₂O₃

Products

Catalogue NumberPackaging Qty/Pack
521231-1MG Plastic ampoule 1 mg
Description
OverviewA cell-permeable bis(1H-2-indolyl)-1-methanone compound that acts as a highly selective, ATP-competitive and reversible inhibitor of platelet-derived growth factor (PDGF) receptor tyrosine kinase (IC50 = 1.1 µM in Swiss 3T3 cells for PDGFR). Also potently inhibits Flt3 (Fms-like tyrosine kinase 3) activity (IC50 = 6.2 µM for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells). Sensitizes 32D cells to radiation-induced apoptosis and inhibits proliferation of TEL-Flt3-transfected BA/F3 cells (IC50 < 300 nM). May also serve as a prodrug form of the Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I (Cat. No. 521230) in cells.
Catalogue Number521231
Brand Family Calbiochem®
Synonyms(5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476
References
ReferencesMahboobi, S., et al. 2002. J. Med. Chem. 45, 1002.
Teller, S., et al. 2002. Leukemia 16, 1528.
Product Information
CAS number249762-74-1
ATP CompetitiveY
FormYellow solid
Hill FormulaC₂₁H₁₈N₂O₃
Chemical formulaC₂₁H₁₈N₂O₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPDGFR in swiss 3T3 cells
Primary Target IC<sub>50</sub>1.1 µM inhibiting PDGFR in swiss 3T3 cells; 6.2 µ M for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells
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 +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
521231-1MG 04055977271355

Documentation

PDGFR Tyrosine Kinase Inhibitor II - CAS 249762-74-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PDGFR Tyrosine Kinase Inhibitor II - CAS 249762-74-1 - Calbiochem Certificates of Analysis

TitleLot Number
521231

References

Reference overview
Mahboobi, S., et al. 2002. J. Med. Chem. 45, 1002.
Teller, S., et al. 2002. Leukemia 16, 1528.
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
Synonyms(5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476
DescriptionProdrug form of Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I (Cat. No. 521230) that acts as a highly selective, cell-permeable, ATP-competitive, and reversible inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine kinase (IC50 = 1.1 µM, Swiss 3T3 cells). Also potently inhibits Fms-like tyrosine kinase 3 (Flt3) activity (IC50 = 6.2 µM for PDGFRβ-mFlt3 and 50 nM in EOL-1 cells). Reported to sensitize 32D cells to radiation-induced apoptosis. Also shown to inhibit proliferation of TEL-Flt3-transfected BA/F3 cells (IC50 > 300 nM).
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number249762-74-1
Chemical formulaC₂₁H₁₈N₂O₃
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (5 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
ReferencesMahboobi, S., et al. 2002. J. Med. Chem. 45, 1002.
Teller, S., et al. 2002. Leukemia 16, 1528.