TAS6417

SKU: orb1307699

Description

Zipalertinib (TAS6417, CLN-081) is a potent, orally bioavailable covalent EGFR inhibitor targeting the ATP-binding hinge region with low nM IC50 values. It is a research tool for investigating EGFR-driven cancers, demonstrating activity in both cellular assays and in vivo tumor models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1661854-97-2
• MW: 396.44
• Purity: 99.71% (May vary between batches)
• Formula: C₂₃H₂₀N₆O
• SMILES: CC1=C[C@@H](Cn2c1c(-c1cnc3ccccc3c1)c1c(N)ncnc21)NC(=O)C=C
• Target: EGFR,Apoptosis
• Solubility: DMSO:55 mg/mL (138.73 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (6.31 mM)

Bioactivity

• Target IC50:
  EGFR:1.1-8.0 nM
• In Vivo:
  METHODS: Nude mice bearing NIH/3T3 EGFR G719A allografts, nude mice bearing BID007, and nude mice bearing H1975 cells were treated with TAS6417 (50, 100, 200 mg/kg, oral, 15 days) to study the in vivo efficacy of Zipalertinib (TAS6417, CLN-081) against EGFR mutations. RESULTS Zipalertinib (TAS6417, CLN-081) inhibited tumor formation in nude mice bearing H1975, NIH/3T3 expressing G719A, NIH/3T3 expressing G719A+T790M, BID007, and H1975-insSVD.
• In Vitro:
  METHODS: Two cell lines with EGFR exon 20 insertion isolated and established from lung cancer patients, BID007 and BID019, were treated with Zipalertinib (TAS6417, CLN-081) (0.001, 0.01, 0.1, 1, 10 μM). RESULTS Zipalertinib (TAS6417, CLN-081) inhibited EGFR phosphorylation in both cell lines at 10 nM and 100 nM.

Storage & Handling

• Storage: keep away from direct sunlight | 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

lung, inhibit, PC-9, NSCLC, H1975, ErbB-1, Epidermal growth factor receptor, EGFR, HER1, Inhibitor, Akt, Apoptosis, BID007, BID019, BEAS-2B, cancer, CLN081, CLN-081, CLN 081, TAS6417, TAS-6417, TAS 6417

Compound Identifiers

PubChem CID

117918742