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

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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 demonstrates 50 fold greater selectivity for EGFR compared to 72 other kinases.
Theliatinib (HMPL-309) EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 442.51

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Quality Control

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

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

Solubility

In vitro
Batch:

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

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In vivo
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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.

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 gefitinib, 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-tumour activity in tumours 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 tumour cells with wild-type EGFR (A431, H292, FaDu cells).
In vivo

Theliatinib (HMPL-309) demonstrates dose-dependent anti-tumour activity in a panel of PDECX (patient-derived oesophageal cancer xenograft) models with a generally good correlation between EGFR H score and tumour growth inhibition. Furthermore, aberrant activation or gene mutations of other targets such as PI3K and FGFR diminish the anti-tumour activity of EGFR TKIs, especially this compound.
References

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