Home Protein Tyrosine Kinase EGFR inhibitor Theliatinib (HMPL-309) For research use only.

Theliatinib (HMPL-309)

Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.

Theliatinib (HMPL-309) Chemical Structure

Theliatinib (HMPL-309) Chemical Structure

CAS No. 1353644-70-8

Purity & Quality Control

Batch: S858401 DMSO]47 mg/mL]false]]]false]]]false Purity: 99.96%
99.96

Theliatinib (HMPL-309) Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Biological Activity

Description Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.
Targets
WT EGFR [1]
(Cell-free assay)		 EGFR T790M/L858R [1]
(Cell-free assay)
3 nM 22 nM
In vitro
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)[1].
Cell Research Cell lines A431 cells
Concentrations 0.005-10 μM
Incubation Time 48 h
Method

A431 cells (1 × 104 cells/well) in exponential phase are seeded in duplicates in DMEM containing 10% FBS and incubated at 37°C and 5% CO2 overnight. Then, 10 μL of test compounds (theliatinib, gefitinib and erlotinib) at tested concentrations (10~0.005 μM, 3 fold gradient dilution) are added into each well with the final concentration of DMSO at 0.5%. The cells are incubated for 48 h followed by further incubation for 1h after adding 10 μL/well CCK-8 solution. Cell survival is determined by measuring the optical density at 450 nm.
In Vivo
In vivo

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[1].
Animal Research Animal Models Seven to nine week old NOD-SCID immunodeficient or BALB/cASlac-nu/nu male or female mice (Tumor-bearing mice)
Dosages 15 mg/kg/day
Administration oral

Chemical Information & Solubility

Molecular Weight 442.51 Formula

C25H26N6O2
CAS No. 1353644-70-8 SDF --
Smiles COC1=C(NC(=O)N2CC3CCN(C)C3C2)C=C4C(=NC=NC4=C1)NC5=CC(=CC=C5)C#C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 47 mg/mL ( (106.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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