Theliatinib (HMPL-309)

Names

[ Name ]:
Theliatinib (HMPL-309)

[Synonym ]:
(3aR,6aR)-N-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yl)-1-methyl-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide
HMPL-309

Biological Activity

[Description]:

Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

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

[Target]

IC50: 3 nM (EGFR), 22 nM (EGFR T790M/L858R)[1] Ki: 0.05 nM (EGFR)[1]

[References]

[1]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₆N₆O₂

[ Molecular Weight ]:
442.52

Theliatinib (HMPL-309)

Names

Biological Activity

Chemical & Physical Properties

Related Compounds