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Merck

676481

VEGFR Tyrosine Kinase Inhibitor II

The VEGFR Tyrosine Kinase Inhibitor II, also referenced under CAS 269390-69-4, controls the biological activity of VEGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

VEGFR Tyrosine Kinase Inhibitor II, N-(4-Chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamide, VEGF Receptor Tyrosine Kinase Inhibitor II, VEGFR2 Kinase Inhibitor XVII, VEGFR1 Kinase Inhibitor III

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About This Item

Empirical Formula (Hill Notation):
C19H16ClN3O
CAS Number:
Molecular Weight:
337.80
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 5 mg/mL, methanol: soluble

shipped in

wet ice

storage temp.

−20°C

SMILES string

Clc1ccc(cc1)NC(=O)c2c(cccc2)NCc3ccncc3

InChI

1S/C19H16ClN3O/c20-15-5-7-16(8-6-15)23-19(24)17-3-1-2-4-18(17)22-13-14-9-11-21-12-10-14/h1-12,22H,13H2,(H,23,24)

InChI key

GGPZCOONYBPZEW-UHFFFAOYSA-N

General description

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC50 = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC50 = 7.0 µM and 7.3 µM). Also displays antiangiogenic and antitumor properties. Does not inhibit the activities of CDK-1, c-Met, IGF-1R or PKA (IC50 >10 µM).
A pyridinyl-anthranilamide compound that displays both antiangiogenic and antitumor properties. A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC50 = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC50 = 7 µM and 7.3 µM). Further, inactive towards the inhibition of CDK-1, c-Met, IGF-1R and PKA (IC50 >10 µM).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Kinase activities of KDR, Flt-1 and c-Kit
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM, 180 nM and 240 nM against kinase activities of KDR, Flt-1 and c-Kit, respectively

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

Furet, P., et al. 2003. Bioorg. Med. Chem. Lett.13, 2967.

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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