Theliatinib

SKU: orb1299921

Description

Theliatinib is a potent and highly selective EGFR inhibitor, exhibiting a Ki of 0.05 nM for wild-type EGFR. It demonstrates anti-tumor activity in research models, with IC50 values of 3 nM and 22 nM against EGFR and the EGFR T790M/L858R mutant, respectively. This compound is applied in preclinical oncology research for investigating EGFR-driven cancers both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1353644-70-8
• MW: 442.51
• Purity: 99.67% (May vary between batches)
• Formula: C₂₅H₂₆N₆O₂
• SMILES: [H][C@]12CCN(C)[C@@]1([H])CN(C2)C(=O)Nc1cc2c(Nc3cccc(c3)C#C)ncnc2cc1OC
• Target: EGFR
• Solubility: DMSO:47 mg/mL (106.21 mM)

Bioactivity

• Target IC50:
  EGFR:0.05 nM (Ki)|EGFR:3 nM (IC50)|EGFR (L858R/T790M):22 nM (IC50)
• In Vivo:
  In vivo data demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431, Bcap-37 and Fadu. Two PDECX models with EGFR gene amplification (PDECX1T0326 and PDECX1T0950) were sensitive to theliatinib treatment demonstrating tumor regression of 32% and 75%, respectively.
• In Vitro:
  In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity.
• Animal Research:
  Seven- to nine week old NOD-SCID immunodeficient or BALB/cASlac-nu/nu male or female mice. Fresh tumor specimens from newly diagnosed patients were collected during surgery and separated into three parts for the following: (1) To prepare formalin fixed paraffin embedded (FFPE) sections; (2) For snap freezing in liquid nitrogen for DNA extraction and sequencing and (3) For subcutaneous implantation into NOD-SCID mice (P0) and subsequent passages in additional NOD-SCID or nude mice once the tumor size reached 800~1500 mm^3. After several consecutive in vivo passages, the PDECX models (P3~P7) were used to evaluate the anti-tumor efficacy of theliatinib or gefitinib or AZD4547.

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

HMPL309, HMPL-309, HMPL 309, Inhibitor, HER1, ERK, esophageal, ErbB-1, Epidermal growth factor receptor, EGFR, inhibit, orally, anti-tumor, ATP-competitive, cancer, AKT, Theliatinib, Xiliertinib, phosphorylation

Compound Identifiers

PubChem CID

54759275