Theliatinib (HMPL-309) - 96%, high purity , CAS No.1353644-70-8, Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of LCK proto-oncogene; Src family tyrosine kinase;Inhibitor of LYN proto-oncogene; Src family tyrosine kinase;Inhibitor of tyrosine kinase non receptor

Item Number

T414072

• Synonyms: Theliatinib|1353644-70-8|6ZZ3B7NZ0B|HMPL-309|UNII-6ZZ3B7NZ0B|(3aR,6aR)-N-(4-((3-Ethynylphenyl)amino)-7-methoxy-6-quinazolinyl)hexahydro-1-methylpyrrolo(3,4-b)pyrrole-5(1H)-carboxamide|(3aR,6aR)-N-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]-1-methyl-2,
• Specifications & Purity: 96%
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of LCK proto-oncogene; Src family tyrosine kinase;Inhibitor of LYN proto-oncogene; Src family tyrosine kinase;Inhibitor of tyrosine kinase non receptor

Product Description

Targets

WT EGFR (Cell-free assay); EGFR T790M/L858R (Cell-free assay) 3 nM; 22 nM

In vitro

In comparison to erlotinib or gefitnib, theliatinib shows much stronger binding affinity to wild type EGFR and is more difficult to be replaced by ATP. This unique feature may result in better target engagement for theliatinib compared to erlotinib or gefitinib, leading to stronger anti-tumor activity in tumors with wild type EGFR activation due to gene amplification or protein overexpression. Theliatinib inhibits EGFR phosphorylation with an IC50 of 0.007 μM for EGF stimulated EGFR phosphorylation in A431 cells and cell survival in tumor cells with wild-type EGFR (A431, H292, FaDu cells).

Theliatinib demonstrates dose-dependent anti-tumor activity in a panel of PDECX (patient-derived esophageal cancer xenograft) models with a generally good correlation between EGFR H score and tumor growth inhibition. Furthermore, aberrant activation or gene mutations of other targets such as PI3K and FGFR diminishes the anti-tumor activity of the EGFR TKIs, especially, theliatinib.

Cell Research(from reference)

Cell lines：A431 cells 

Concentrations：0.005-10 μM 

Incubation Time：48 h