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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
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
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)
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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