Home Protein Tyrosine Kinase EGFR inhibitor Theliatinib (HMPL-309)

research use only

Theliatinib (HMPL-309) EGFR inhibitor

Cat.No.S8584

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) EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 442.51

Jump to

Quality Control

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

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (106.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 442.51 Formula

C25H26N6O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1353644-70-8 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(NC(=O)N2CC3CCN(C)C3C2)C=C4C(=NC=NC4=C1)NC5=CC(=CC=C5)C#C

Mechanism of Action

Targets/IC50/Ki
WT EGFR
(Cell-free assay)
3 nM
EGFR T790M/L858R
(Cell-free assay)
22 nM
In vitro

In comparison to erlotinib or gefitnib, theliatinib (HMPL-309) 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 this compound 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. It 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).
In vivo

Theliatinib (HMPL-309) 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 diminish the anti-tumor activity of EGFR TKIs, especially this compound.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map