Home Protein Tyrosine Kinase EGFR inhibitor Pyrotinib dimaleate

research use only

Pyrotinib dimaleate EGFR inhibitor

Cat.No.S8852

Pyrotinib dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.
Pyrotinib dimaleate EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 815.22

Jump to

Quality Control

Batch: Purity: 99.88%
99.88

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (122.66 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : 16 mg/mL

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 815.22 Formula

C40H39ClN6O11

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1397922-61-0 -- Storage of Stock Solutions

Synonyms SHR-1258, BLTN, Pyrroltinib dimaleate Smiles CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CC5CCCN5C

Mechanism of Action

Targets/IC50/Ki
EGFR
(Cell-free assay)
0.013 μM
HER2
(Cell-free assay)
0.038 μM
In vitro

Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.
In vivo

Pyrotinib (SHR1258) displays robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05745740 Not yet recruiting
Non-small Cell Lung Cancer
RemeGen Co. Ltd.
 April 2024 Phase 1|Phase 2
NCT05482568 Recruiting
Advanced Non-small Cell Lung Cancer
Jiangsu HengRui Medicine Co. Ltd.
 September 15 2022 Phase 1|Phase 2
NCT04850651 Completed
Healthy Subjects
Jiangsu HengRui Medicine Co. Ltd.
 April 16 2021 Phase 1
NCT04680091 Unknown status
Healthy Subjects Drug-drug Interaction Pyrotinib
Jiangsu HengRui Medicine Co. Ltd.
 November 12 2020 Phase 1

Tech Support

Handling Instructions

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

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

Signaling Pathway Map