c-Kit-IN-3

SKU: orb1309887

Description

c-Kit-IN-3 is a potent and selective c-KIT kinase inhibitor, demonstrating IC50 values of 4 nM against wild-type and 8 nM against the T670I mutant. This small molecule is a valuable research tool for investigating c-KIT-driven pathologies, such as gastrointestinal stromal tumors (GIST), in both cellular and animal model studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2363169-01-9
• MW: 516.9
• Purity: 99.94% (May vary between batches)
• Formula: C₂₆H₂₀ClF₃N₂O₄
• SMILES: O(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
• Target: c-Kit
• Solubility: DMSO:100 mg/mL (193.46 mM)

Bioactivity

• Target IC50:
  c-Kit (WT):4 nM |c-Kit (T670I):8 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c Kit IN 3, cKit, c-Kit, c-KIT w, cKitIN3, c-Kit-IN-3, c-KIT T670I

Compound Identifiers

PubChem CID

139030518