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
• Empirical Formula (Hill Notation): C₂₁H₁₈N₂O₃
• CAS Number: 249762-74-1
• Molecular Weight: 346.38
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

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

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable