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c-Kit-IN-3

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Catalog No. T10651Cas No. 2363169-01-9

c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I).

c-Kit-IN-3

c-Kit-IN-3

🥰Excellent
Purity: 99.43%
Catalog No. T10651Cas No. 2363169-01-9
c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I).
Pack SizePriceAvailabilityQuantity
1 mg75 €In Stock
5 mg156 €In Stock
10 mg253 €In Stock
25 mg418 €In Stock
50 mg562 €In Stock
100 mg786 €In Stock
500 mg1.577 €In Stock
1 mL x 10 mM (in DMSO)334 €In Stock
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Purity:99.43%
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Product Introduction

Bioactivity
Description
c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I).
Targets&IC50
c-Kit (WT):4 nM , c-Kit (T670I):8 nM
In vitro
In primary GIST patient cells, c-Kit-IN-3 (0.1-10 μM) exhibits dose-dependent antiproliferative effects. In GIST-T1, GIST-T1-T670I, and GIST-5R cells, c-Kit-IN-3 (0.01-1 μM) induces dose-dependent cell apoptotic death and arrests the cell cycle into the G0/G1 phase[1].
In vivo
c-Kit-IN-3 (1 mg/kg i.v. for mice, rats, dog; 10 mg/kg p.o. for mice, rats; 5 mg/kg p.o. for dog) has T1/2 of 4.5 h, 6.4 h, 19.4 h for mice, rats and dogs, respectively. c-Kit-IN-3 possesses acceptable bioavailability of 43%, 50% and 81% for mice, rats, and dogs. In female BALB/C-nu mice, c-Kit-IN-3 (20-100 mg/kg; gavage) treatment dose-dependently inhibits the tumor progression[1].
Chemical Properties
Molecular Weight516.9
FormulaC26H20ClF3N2O4
Cas No.2363169-01-9
SmilesO(C=1C2=C(C=C(OC)C(OC)=C2)N=CC1)C3=CC=C(NC(CC4=CC(C(F)(F)F)=C(Cl)C=C4)=O)C=C3
Relative Density.1.379 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (193.46 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9346 mL9.6731 mL19.3461 mL96.7305 mL
5 mM0.3869 mL1.9346 mL3.8692 mL19.3461 mL
10 mM0.1935 mL0.9673 mL1.9346 mL9.6731 mL
20 mM0.0967 mL0.4837 mL0.9673 mL4.8365 mL
50 mM0.0387 mL0.1935 mL0.3869 mL1.9346 mL
100 mM0.0193 mL0.0967 mL0.1935 mL0.9673 mL

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