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

c-Kit-IN-3 

Cat. No.: HY-128704
Handling Instructions

c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.

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

c-Kit-IN-3 Chemical Structure

c-Kit-IN-3 Chemical Structure

CAS No. : 2363169-01-9

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10 mM * 1 mL in DMSO USD 136 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 800 In-stock
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100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops[1].

IC50 & Target

IC50: 4 nM (c-KIT w) and 8 nM (c-KIT T670I)[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 (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 (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 (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 potently inhibits the activity of CSF1R (IC50: 18 nM), PDGFRα (IC50: 25 nM), RET (IC50: 34 nM), and it relatively less potently inhibits DDR1 (IC50: 135 nM), FLT4 (IC50: 121 nM), and PDGFRβ (IC50: 97 nM)[1].
c-Kit-IN-3 (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 Proliferation 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.

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.

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 cells apoptotic death.

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: 24 hours
Result: Decreased the autophosphorylation of c-KIT pY703, pY719, and pY823 in GIST-T1, GIST-T1-T670I, and GIST-5R cells, respectively.
In Vivo

c-Kit-IN-3 (Compound 18; oral gavage; 20-100 mg/kg/day; for 11 days; female BALB/C-nu mice) treatment dose dependently inhibits the tumor progression[1].
c-Kit-IN-3 (1 mg/kg (iv for mice, rats, dog); 10 mg/kg (p.o. for mice, rats ) and 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. And it possesses acceptable bioavailability in mice (F = 43%), rats (F = 50%), and dogs (F = 81%)[1].

Animal Model: Female BALB/C-nu mice[1]
Dosage: 20 mg/kg, 40 mg/kg, 80 mg/kg, 100 mg/kg
Administration: Oral gavage; daily; for 11 days
Result: Dose dependently inhibited the tumor progression.
Animal Model: Mice, Sprague Dawley Rats, and Beagle Dogs[1]
Dosage: 1 mg/kg (iv for mice, rats, dog); 10 mg/kg (p.o. for mice, rats ) and 5 mg/kg (p.o. for dog) (Pharmacokinetic Analysis)
Administration: Iv or p.o.
Result: Had T1/2 of 4.5 h, 6.4 h, 19.4 h for mice, rats and dogs, respectively. And it possessed acceptable bioavailability in mice (F = 43%), rats (F = 50%), and dogs (F = 81%).
Molecular Weight

516.90

Formula

C₂₆H₂₀ClF₃N₂O₄

CAS No.

2363169-01-9

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

c-Kit-IN-3c-KitSCFRCD117Inhibitorinhibitorinhibit

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