EGFR-IN-7

SKU: orb1219627

Description

EGFR-IN-7 is a selective and potent EGFR kinase inhibitor.TQB3804 displayed potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM respectively, and has similar enzymatic activity for EGFRWT (IC50 = 1.07) to Osimertinib. It also showed expected anti-proliferative activity in 4 cell lines, Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), PC9 (EGFRd746-750), and A431 (EGFRWT), with IC50 of 26.8, 163, 45, and 147 nM, respectively.

Key Properties

• CAS Number: 2267329-76-8
• MW: 694.6
• Purity: >98% (HPLC)
• Formula: C₃₂H₄₁BrN₉O₂P
• SMILES: COc1cc(N2CCC(CC2)N2CCN(C)CC2)c(C)cc1Nc1ncc(Br)c(Nc2ccc3nccnc3c2P(C)(C)=O)n1
• Target: EGFR
• Solubility: DMSO:5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCL and heat to 60°C)

Bioactivity

• In Vivo:
  EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o. ; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model. EGFR-IN-7 (25 and 50 mg/kg; p.o. ; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model. Animal model: Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g). Dosage: 5, 15, 45 mg/kg. Administration: Oral administration, daily, for 13 days. Result: Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice. Animal model: Subcutaneous xenograft PC-9 (Δ19del) model. Dosage: 0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg. Administration: Oral administration, once a day, 3 weeks. Result: Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.
• In Vitro:
  EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively. EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM. EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM. EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM. Cell Proliferation Assay Cell line: A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) suspension cells. Concentration: 1 mM; 10 μM-0.508 nM Incubation time: 3 days. Result: Inhibited proliferation in cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TQB3804

Quick Database Links

Gene Symbol

EGFR