Simotinib hydrochloride

Names

[ Name ]:
Simotinib hydrochloride

Biological Activity

[Description]:

Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

EGFR:19.9 nM (pIC50)

[In Vitro]

Simotinib hydrochloride inhibits in a dose-dependent manner EGFR and the growth of human A431 tumor cells with high expression of EGFR, with no significant activity on other investigated kinases[1].

[In Vivo]

Simotinib hydrochloride has been shown to exert its antitumor activity by inhibiting EGFR phosphorylation in nude xenograft model[1].

[References]

[1]. Hu XS, et al. Safety, tolerability, and pharmacokinetics of simotinib, a novel specific EGFR tyrosine kinase inhibitor, in patients with advanced non-small cell lung cancer: results of a phase Ib trial. Cancer Manag Res. 2019;11:4449-4459. Published 2019 May 13.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₇Cl₂FN₄O₄

[ Molecular Weight ]:
537.41

Simotinib hydrochloride

Names

Biological Activity

Chemical & Physical Properties

Related Compounds