Tarloxotinib bromide

SKU: orb1309032

Description

Tarloxotinib bromide

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1636180-98-7
• MW: 681.77
• Purity: 99.52%
• Formula: C₂₄H₂₄Br₂ClN₉O₃
• SMILES: [Br-].Cn1cnc(c1C[N+](C)(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(Cl)c(Br)c3)ncnc2cn1)[N+]([O-])=O
• Target: EGFR,HER
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.93 mM);DMSO:33 mg/mL (48.4 mM)

Bioactivity

• In Vivo:
  Tarloxotinib bromide treatment regresses the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo.
• In Vitro:
  Tarloxotinib bromide is metabolized efficiently under hypoxia using a panel of human NSCLC cell lines (rate of TKI release 0.4-2.1 nM/hr/106 cells), a process that is inhibited by oxygen (TKI release <0.002 nM/hr/106 cells). Cellular anti-proliferative and receptor phosphorylation assays demonstrate a 14-80 fold reduction of Tarloxotinib bromide activity relative to TKI. Using PC9 tumors, hyperbaric oxygen breathing suppresse release of TKI from Tarloxotinib bromide by >80% (538 vs 99 nM/kg; p<0.01) compared to air breathing controls.

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

Tarloxotinib, Tarloxotinib bromide, Tarloxotinib Bromide, TH4000, TH-4000, TH 4000, inhibit, ErbB-1, EGFR, Epidermal growth factor receptor, EGFR/HER2, Inhibitor, HER1, HER2

Compound Identifiers

PubChem CID

51038315