Tuxobertinib

SKU: orb1298393

Description

Tuxobertinib (BDTX-189) is a highly selective, allosteric inhibitor targeting oncogenic mutations in EGFR and HER2, demonstrating potent anticancer activity. It has shown efficacy in preclinical in vitro and in vivo models for non-small cell lung cancer and other solid tumors driven by these mutations.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2414572-47-5
• MW: 561.03
• Purity: 99.22%
• Formula: C₂₉H₂₉ClN₆O₄
• SMILES: Clc1cc(Nc2ncnc3cc(OCCN4CCOCC4)c(NC(=O)C=C)cc23)ccc1OCc1ccccn1
• Target: HER,RIP kinase,EGFR,BTK
• Solubility: DMSO:41.67 mg/mL (74.27 mM)

Bioactivity

• Target IC50:
  EGFR:0.2 nM(KD)|BLK:13 nM(KD)|HER2:0.76 nM(KD)|RIPK2:1.2 nM(KD)
• In Vivo:
  BDTX-189 (0-100 mg/kg; p.o.; daily for 15 dyas) shows dose-dependent tumor growth inhibition and regression in in athymic nude mice bearing HER2 S310F Ba/F3 allograft tumors. BDTX-189 (1-50 mg/kg.p.o.; daily for 15 days) shows dose-dependent tumor growth inhibition and regression in athymic nude mice bearing CUTO-14 PDX tumors that express the EGFR mutation EGFR ASV

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

Ba/F3, BLK, BDTX 189, BDTX189, BDTX-189, allosteric, mice, oral, oncogene athymic, nude, inhibit, mutants, HER1, HER2, Inhibitor, insertion, EGFR, Epidermal growth factor receptor, ErbB-1, RIP kinase, RIPK2, RIPkinase, Tuxobertinib

Compound Identifiers

PubChem CID

154824631