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Merck

676503

VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor

The VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor controls the biological activity of VEGFR/Tie-2/PDGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor, 1-(2-Fluoro-4-((5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea, PDGFR Tyrosine Kinase Inhibitor XXI, VEGFR Tyrosine Kinase Inhibitor XXXIV, VEGFR2 Kinase Inhibitor XXXII, VEGFR1 Kinase Inhibitor VII

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About This Item

Empirical Formula (Hill Notation):
C21H15F4N5O2
CAS Number:
919279-04-2
Molecular Weight:
445.37
UNSPSC Code:
12352200
MDL number:
MFCD25977022
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

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SMILES string

O=C(NC1=CC(C(F)(F)F)=CC=C1)NC2=CC=C(OC3=NC=NC4=C3N(C)C=C4)C=C2F

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

light beige

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

General description

An orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRα, PDGFRβ and c-kit (IC50 = 6.2, 15, 20, 35, 96 and 170 nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50 = 0.9 and 1.05 µM) and FGFR1, HER2, EGFR, IR, PKCθ (>10 µM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50 = 4.4 µM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6 mg/kg, b.i.d.).

Other Notes

Oguro, Y., et al. 2010. Bioorg. Med. Chem.18, 7150.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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