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c-Kit-IN-3

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Purity:99.43%

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COA HNMR HPLC

c-Kit-IN-3

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).

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Pack Size	Price	Availability
1 mg	$79	In Stock
5 mg	$165	In Stock
10 mg	$267	In Stock
25 mg	$441	In Stock
50 mg	$592	In Stock
100 mg	$828	In Stock
500 mg	$1,660	In Stock
1 mL x 10 mM (in DMSO)	$352	In Stock

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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 Weight	516.9
Formula	C26H20ClF3N2O4
Cas No.	2363169-01-9

Storage & Solubility Information

Storage

Powder: -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

	1mg	5mg	10mg	50mg
1 mM	1.9346 mL	9.6731 mL	19.3461 mL	96.7305 mL
5 mM	0.3869 mL	1.9346 mL	3.8692 mL	19.3461 mL
10 mM	0.1935 mL	0.9673 mL	1.9346 mL	9.6731 mL
20 mM	0.0967 mL	0.4837 mL	0.9673 mL	4.8365 mL
50 mM	0.0387 mL	0.1935 mL	0.3869 mL	1.9346 mL
100 mM	0.0193 mL	0.0967 mL	0.1935 mL	0.9673 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

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