Theliatinib (HMPL-309)

Catalog No.S8584

Theliatinib (HMPL-309) Chemical Structure

Molecular Weight(MW): 442.51

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.

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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 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].

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].

Protocol

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Seven to nine week old NOD-SCID immunodeficient or BALB/cASlac-nu/nu male or female mice (Tumor-bearing mice)
  • Formulation: aqueous 0.5% sodium carboxymethyl cellulose (CMC-Na)
  • Dosages: 15 mg/kg/day
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 47 mg/mL (106.21 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 442.51
Formula

C25H26N6O2

CAS No. 1353644-70-8
Storage powder
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID