1. Protein Tyrosine Kinase/RTK
  2. c-Kit
  3. c-Kit-IN-3 maleate

c-Kit-IN-3 maleate 

Cat. No.: HY-128704A4
Handling Instructions

c-Kit-IN-3 maleate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50 of 4 nM. c-Kit-IN-3 maleate displays great potencies against c-KIT kinase and a broad spectrum of drug-resistant mutants in the biochemical assay. c-Kit-IN-3 maleate has improved bioavailability.

For research use only. We do not sell to patients.

c-Kit-IN-3 maleate Chemical Structure

c-Kit-IN-3 maleate Chemical Structure

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Description

c-Kit-IN-3 maleate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50 of 4 nM. c-Kit-IN-3 maleate displays great potencies against c-KIT kinase and a broad spectrum of drug-resistant mutants in the biochemical assay. c-Kit-IN-3 maleate has improved bioavailability[1].

IC50 & Target

IC50: 4 nM (c-KIT kinase)[1]

In Vitro

c-Kit-IN-3 (Compound 18; 0.1-10 μM; 6 days; primary GIST patient cells) exhibits dose-dependent antiproliferative effects[1].
c-Kit-IN-3 (Compound 18; 0.01-1 μM; 24 hours; GIST-T1, GIST-T1-T670I, and GIST-5R cells) treatment induces dose-dependent cell apoptotic death (by examining the cleaved PARP and cleaved caspase 3)[1].
c-Kit-IN-3 (Compound 18; 0.01-1 μM; 24 hours; GIST-T1, GIST-T1-T670I, and GIST-5R cells) treatment arrests the cell cycle into the G0/G1 phase in all of these three cell lines[1].
c-Kit-IN-3 (Compound 18; 0-1 μM; 24 hours) blocks the autophosphorylation of c-KIT pY703, pY719, and pY823 in GIST-T1, GIST-T1-T670I, and GIST-5R, respectively, cells at a concentration of 30 nM and inhibits the downstream signaling mediators pAKT (T308/S473), pS6 (S235/236), and pERK (T202/204)[1].
  c-Kit-IN-3 (Compound 18; 0.006 μM-1.37 μM) potently inhibits the growth of c-KIT-dependent GIST cancer cells, such as GIST-T1 (IC50: 0.006 μM); GIST-882 (IC50: 0.013 μM); GIST-T1-T670I (IC50 : 0.011 μM); GIST-5R (IC50: 0.073 μM); GIST-48B (IC50: 1.37 μM), respectively[1].

Cell Viability Assay[1]

Cell Line: Primary GIST patient cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 6 days
Result: Inhibition of the proliferation of primary GIST patient cells.

Apoptosis Analysis[1]

Cell Line: GIST-T1, GIST-T1-T670I, and GIST-5R cells
Concentration: 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM
Incubation Time: 24 hours
Result: Induced dose-dependent cell apoptotic death.

Cell Cycle Analysis[1]

Cell Line: GIST-T1, GIST-T1-T670I, and GIST-5R cells
Concentration: 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle into the G0/G1 phase in all of these three cell lines.

Western Blot Analysis[1]

Cell Line: GIST-T1, GIST-T1-T670I, and GIST-5R cells
Concentration: 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM
Incubation Time: 2 hours
Result: Blocked the autophosphorylation of c-KIT pY703, pY719, and pY823 in GIST-T1, GIST-T1-T670I, and GIST-5R, respectively, cells at a concentration of 30 nM and also remarkably inhibited the downstream signaling mediators pAKT (T308/S473), pS6 (S235/236), and pERK (T202/204) (EC50 less than 100 nM). Also significantly affected the phosphorylation of cKIT pY703, pY719, and pY823 and downstream mediators (EC50 less than 100 nM). Strongly inhibited the phosphorylation of STAT3 in GIST-T1-T670I and GIST-5R cells but moderately in GIST-T1 cells.
In Vivo

c-Kit-IN-3 (Compound 18; 40-100 mg/kg; oral gavage; daily; for 11 days; for 4 weeks; female BALB/C-nu mice) treatment dose dependently inhibits the BaF3-tel-c-KIT-T670I tumor progression and exhibited almost 100% TGI (tumor growth inhibition) at a dosage of 100 mg/kg/day. And do not affect the animal weights[1].

Animal Model: Female BALB/C-nu mice bearing established BaF3-tel-c-KIT-T670I tumor xenografts[1]
Dosage: 40 mg/kg, 100 mg/kg
Administration: Oral gavage; daily; for 11 days
Result: Dose dependently inhibited the BaF3-tel-c-KIT-T670I tumor progression and exhibited almost 100% TGI (tumor growth inhibition) at a dosage of 100 mg/kg/day.
Molecular Weight

632.97

Formula

C₃₀H₂₄ClF₃N₂O₈

SMILES

O=C(O)/C=C\C(O)=O.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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

c-Kit-IN-3c-KitSCFRCD117Inhibitorinhibitorinhibit

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c-Kit-IN-3 maleate
Cat. No.:
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