PDGFR Tyrosine Kinase Inhibitor II

Name: PDGFR Tyrosine Kinase Inhibitor II
Brand: MM

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

Select a Size

All Photos(1)

About This Item

Empirical Formula (Hill Notation):

C₂₁H₁₈N₂O₃

CAS Number:

249762-74-1

Molecular Weight:

346.38

MDL number:

MFCD24710161

NACRES:

NA.77

UNSPSC Code:

12352200

Product Name

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.

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

Quality Level

100

Related Categories

Bioactive Small Molecule Inhibitors

Legal Information

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

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

Disclaimer

Toxicity: Standard Handling (A)

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).

Other Notes

Mahboobi, S., et al. 2002. J. Med. Chem.45, 1002.
Teller, S., et al. 2002. Leukemia16, 1528.

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.

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c