Larotinib

SKU: orb1744254

Description

Larotinib is a potent, orally bioavailable broad-spectrum tyrosine kinase inhibitor, exhibiting high potency against EGFR with an IC50 of 0.6 nM. It is utilized in cancer research for investigating oncogenic signaling pathways in both cellular and animal models of EGFR-driven malignancies.

Research Area

Cardiovascular Research, Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1438072-11-7
• MW: 488.94
• Purity: 99.73%
• Formula: C₂₄H₂₆ClFN₄O₄
• SMILES: N(C=1C2=C(C=C(OC)C(OCCCN3C[C@@]4([C@](C3)(OCCO4)[H])[H])=C2)N=CN1)C5=CC(Cl)=C(F)C=C5
• Target: BTK,IRAK,Tyrosine Kinases,EGFR
• Solubility: DMSO:60 mg/mL (122.71 mM)

Bioactivity

• Target IC50:
  HER4:84 nM|EGFR (L858R):0.563 nM|HER2:253 nM|IRAK1:167 nM|BTK:196 nM|EGFR (T790M):45.2 nM|EGFR (WT):0.611 nM|BLK:102 nM|EGFR (L861Q):0.423 nM
• In Vivo:
  Larotinib (250, 300, 350 mg; oral; once daily; patients) demonstrated promising antitumor activity and manageable safety profiles in patients with pre-treated advanced ESCC with EGFR overexpression or amplification, especially at the dose of 350 mg, which showed better efficacy and acceptable safety. A phase 3 study is underway on 350 mg larotinib in ESCC patients with EGFR overexpression.

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

Tyrosine Kinases, TyrosineKinases, BTK, IRAK, EGFR

Compound Identifiers

PubChem CID

89584422