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c-KIT-IN-3 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752842

c-Kit-IN-3 is a potent and selective c-KIT kinase inhibitor (IC50s: 4nM, 8nM for c-KIT wt, and c-KIT T670I). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
PDF
QC Report View PDF
PDF
Material Safety Data Sheet View PDF
PDF
Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
c-Kit-IN-3, Inhibitor
Full Product Name
c-Kit-IN-3
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
516.9
Solubility
DMSO: 100mg/mL (193.46mM)
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C26H20ClF3N2O4
SMILES
O=C(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1)CC4=CC=C(Cl)C(C(F)(F)F)=C4
CAS Number
2363169-01-9
Target & IC50
c-KIT w: ic50 4nM
c-KIT T670I: ic50 8nM
In Vitro
c-Kit-IN-3 (oral gavage; 20-100mg/kg/day; for 11 days; female BALB/C-nu mice) treatment,dose-dependently inhibits the tumor progression. c-Kit-IN-3 (1mg/kg iv for mice, rats, dog; 10mg/kg p.o. for mice, rats; and 5mg/kg p.o. for dog) has T1/2 of 4.5 h, 6.4 h, 19.4 h for mice, rats and dogs, respectively. And it possesses acceptable bioavailability in mice (F = 43%), rats (F = 50%), and dogs (F = 81%).

Product References and Citations for c-Kit-IN-3, inhibitor

Wu Y, et al. Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. J Med Chem. 2019 Jul 11;62(13):6083-6101.
Wu Y, et al. Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. J Med Chem. 2019 Jul 11;62(13):6083-6101.

Other Notes

Small volumes of c-Kit-IN-3, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for c-Kit-IN-3 purchase

MBS5752842 is an inhibitor targeting c-Kit-IN-3.
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