(Rac)-JBJ-04-125-02

SKU: orb1298564

Description

JBJ-04-125-02 demonstrates efficacy as a monotherapy in EGFR-mutant lung cancer models, both in vitro and in vivo. This small molecule inhibitor is a research tool for studying oncogenic EGFR signaling and evaluating potential therapeutic strategies in preclinical cancer research.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2140807-05-0
• MW: 543.61
• Purity: 95.85%
• Formula: C₂₉H₂₆FN₅O₃S
• SMILES: Oc1ccc(F)cc1C(N1Cc2ccc(cc2C1=O)-c1ccc(cc1)N1CCNCC1)C(=O)Nc1nccs1
• Target: EGFR
• Solubility: DMSO:55 mg/mL (101.18 mM)

Bioactivity

• Target IC50:
  EGFR:0.26 nM
• In Vivo:
  The combination of osimertinib and JBJ-04-125-02 is a significantly more effective treatment approach than either agent alone.
• In Vitro:
  (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M.
• Animal Research:
  Ba/F3, H1975, H3255GR and H3255DR cells were treated with increasing concentrations of inhibitors for 72 hours and growth or the inhibition of growth was assessed by MTS assay according to previously established methods.

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

anti-proliferation, anti-tumor, (Rac) JBJ 04 125 02, (Rac)JBJ0412502, Allosteric, EGFR, EGFR (L858R/T790M), Epidermal growth factor receptor, ErbB-1, Inhibitor, HER1, inhibit, JBJ-04-125-02, T790M-mutant, racemate

Compound Identifiers

PubChem CID

132020316