Epitinib (succinate)

Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer[1][2]. Epitinib (succinate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[2252334-12-4]

Product Name Alternative

HMPL-813 (succinate)

UNSPSC

12352005

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/epitinib-succinate.html

Purity

99.01

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(CCC(O)=O)O.O=C(N1CCN(CC)CC1)NC2=CC3=C(NC4=CC=CC(C#C)=C4)N=CN=C3C=C2OC

Molecular Formula

C28H32N6O6

Molecular Weight

548.59

References & Citations

[1]Zhou et al. The safety profile of a selective EGFR TKI epitinib (HMPL-813) in patients with advanced solid tumors and preliminary clinical efficacy in EGFRm+ NSCLC patients with brain metastasis. Journal of Clinical Oncology 2016 34:15_suppl, e20502-e20502|[2]Zhou et al. Phase I study of the safety and pharmacokinetics of epitinib, an oral EGFR tyrosine kinase inhibitor, in patients with advanced solid tumors. Journal of Clinical Oncology 2013 31:15_suppl, e19042-e19042