Tarloxotinib (bromide)

Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.

Product Specifications

CAS Number

[1636180-98-7]

Product Name Alternative

TH-4000

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tarloxotinib_bromide.html

Purity

98.02

Solubility

DMSO : ≥ 33 mg/mL

Smiles

BrC1=C(Cl)C=CC(NC2=NC=NC3=C2C=C(NC(/C=C/C[N+](C)(C)CC4=C([N+]([O-])=O)N=CN4C)=O)N=C3)=C1.[Br-]

Molecular Formula

C24H24Br2ClN9O3

Molecular Weight

681.77

Precautions

H302, H315, H319, H335

References & Citations

[1]Shevan Silva, Abstract A67: Preclinical efficacy of tarloxotinib bromide (TH-4000), a hypoxia-activated EGFR/HER2 inhibitor: rationale for clinical evaluation in EGFR mutant, T790M-negative NSCLC following progression on EGFR-TKI therapy. Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA.|[2]Adam V. Patterson, Abstract 5358: The hypoxia-activated EGFR-TKI TH-4000 overcomes erlotinib-resistance in preclinical NSCLC models at plasma levels achieved in a Phase 1 clinical trial. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.