TAS0728

SKU: orb1299477

Description

TAS0728

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2088323-16-2
• MW: 504.58
• Purity: 97.78%
• Formula: C₂₆H₃₂N₈O₃
• SMILES: CN(C)C(=O)Cc1ccc(NC(=O)c2nn([C@@H]3CCCN(C3)C(=O)C=C)c3ncnc(N)c23)c(C)c1C
• Target: EGFR,HER
• Solubility: DMSO:125 mg/mL (247.73 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.93 mM)

Bioactivity

• Target IC50:
  HER2 (human):36 nM|JAK3:33 nM|SLK:25 nM|BLK:31 nM|BMX kinase:4.9 nM|LOK:86 nM|HER2:13 nM|EGFR:65 nM|HER4:8.5 nM
• In Vitro:
  TAS0728 exhibited robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors, thereby inducing apoptosis of HER2-amplified breast cancer cells and in tumor tissues of a xenograft model. TAS0728 induced tumor regression in mouse xenograft models bearing HER2 signal-dependent tumors and exhibited a survival benefit without any evident toxicity in a peritoneal dissemination mouse model bearing HER2-driven cancer 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

inhibit, Inhibitor, EGFR, Epidermal growth factor receptor, ErbB-1, HER1, HER2, TAS0728, TAS-0728, TAS 0728

Compound Identifiers

PubChem CID

130275856