Tucatinib

SKU: orb1305592

Description

Tucatinib (ONT-380) is a highly selective small molecule inhibitor of HER2 with an IC50 of 8 nM. It is widely used in preclinical research, including in vitro cell studies and in vivo models, to investigate targeted therapies for HER2-positive cancers such as breast and colorectal malignancies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 937263-43-9
• MW: 480.52
• Purity: 99.96% (May vary between batches)
• Formula: C₂₆H₂₄N₈O₂
• SMILES: Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1
• Target: EGFR,HER
• Solubility: Ethanol:15 mg/mL (31.22 mM);DMSO:45 mg/mL (93.65 mM)

Bioactivity

• Target IC50:
  ErbB2:8 nM
• In Vivo:
  In vivo,Tucatinib significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models. It shows excellent activity in numerous mouse tumor models including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. In the BT-474 model,Tucatinib demonstrated significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size).
• In Vitro:
  Irbinitinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.

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

Tucatinib, ARRY 380, ARRY380, ARRY-380, Inhibitor, HER2/ErbB2, HER1, EGFR, Epidermal growth factor receptor, ErbB-1, inhibit, Irbinitinib, p95 HER2, ONT 380, ONT380, ONT-380

Compound Identifiers

PubChem CID

51039094