Tucatinib hemiethanolate

SKU: orb1693558

Description

Tucatinib hemiethanolate (Irbinitinib hemiethanolate) is a potent, selective, and orally bioavailable HER2 tyrosine kinase inhibitor. It is utilized in preclinical and clinical research for metastatic HER2-positive cancers, including breast and colorectal cancer, demonstrating activity in both in vitro assays and in vivo models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1429755-56-5
• MW: 1007.11
• Purity: 99.76%
• Formula: C₅₄H₅₄N₁₆O₅
• SMILES: CCO.Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1.Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1
• Target: HER,EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (3.28 mM);DMSO:125 mg/mL (124.12 mM)

Bioactivity

• Target IC50:
  HER2:8 nM (IC50)
• In Vivo:
  Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) improves survival at maximum-tolerated dose and reduces brain pErbB2 levels by 80%. This compound (ARRY-380 hemiethanolate) shows significant tumor growth inhibition (TGI)—50% at 50 mg/kg/d and up to 96% at 100 mg/kg/d, with over 50% reduction in baseline tumor size in 9 out of 12 animals at the higher dosage. When combined with trastuzumab at 50 mg/kg/d, it achieves 98% TGI, with complete regressions in 9 out of 12 animals and partial regressions in two.
• In Vitro:
  Tucatinib hemiglycolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 over EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 but not EGFR.

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

ARRY-380 hemiethanolate, HER2, ONT-380 hemiethanolate, Irbinitinib hemiethanolate, Tucatinib

Compound Identifiers

PubChem CID

162623678