Theliatinib (HMPL-309)

Modify Date: 2023-02-06 17:30:29

Theliatinib (HMPL-309) Structure
Theliatinib (HMPL-309) structure
Common Name Theliatinib (HMPL-309)
CAS Number 1353644-70-8 Molecular Weight 442.52
Density N/A Boiling Point N/A
Molecular Formula C25H26N6O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Theliatinib (HMPL-309)


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].

 Names

Name Theliatinib
Synonym More Synonyms

 Theliatinib (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
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

 Synonyms

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