Theliatinib

SKU: orb1220471

Description

Theliatinib a potent and highly selective EGFR inhibitor with anti-tumor activity. Ki of 0.05 nM for wild type EGFR and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant respectively.(In Vivo):Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response.

Key Properties

• CAS Number: 1353644-70-8
• MW: 442.5
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₆N₆O₂
• SMILES: [H][C@]12CCN(C)[C@@]1([H])CN(C2)C(=O)Nc1cc2c(Nc3cccc(c3)C#C)ncnc2cc1OC
• Target: EGFR
• Solubility: DMSO:47 mg/mL (106.21 mM)

Bioactivity

• In Vivo:
  Theliatinib (2-15 mg/kg; oral administration; daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of75% at the end of study, and with a dose response. Animal model: NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model). Dosage: 2 mg/kg, 5 mg/kg, 15 mg/kg. Administration: Oral administration; daily; for 21 days. Result: Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.

Storage & Handling

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

Quick Database Links

Gene Symbol

EGFR