521231
PDGFR Tyrosine Kinase Inhibitor II
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.
Synonym(s):
PDGFR Tyrosine Kinase Inhibitor II, (5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476
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About This Item
Empirical Formula (Hill Notation):
C21H18N2O3
CAS Number:
Molecular Weight:
346.38
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A 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 M in Swiss 3T3 cells for PDGFR). Also potently inhibits Flt3 (Fms-like tyrosine kinase 3) activity (IC50 = 6.2 M 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 in cells.
Prodrug 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).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFR in swiss 3T3 cells
PDGFR in swiss 3T3 cells
Product competes with ATP.
Reversible: yes
Target IC50: 1.1 µM inhibiting PDGFR in swiss 3T3 cells; 6.2 µ M for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Mahboobi, S., et al. 2002. J. Med. Chem.45, 1002.
Teller, S., et al. 2002. Leukemia16, 1528.
Teller, S., et al. 2002. Leukemia16, 1528.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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