1353644-70-8

1353644-70-8 structure

Name: Theliatinib (HMPL-309)
Chemical Name: Theliatinib
CAS Number: 1353644-70-8
Molecular Formula: C₂₅H₂₆N₆O₂
Molecular Weight: 442.52
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2018-06-08 13:55:34
Modify Date: 2024-10-05 08:45:27
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].

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

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.

Molecular Formula	C₂₅H₂₆N₆O₂
Molecular Weight	442.52