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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 Phosphoryl

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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

Key Spec Table

CAS #Empirical Formula
249762-74-1C₂₁H₁₈N₂O₃

Products

Catalogue NumberPackaging Qty/Pack
521231-1MG Plastic ampoule 1 mg
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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
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
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
Global Trade Item Number
Catalogue Number GTIN
521231-1MG 04055977271355