Home Protein Tyrosine Kinase EGFR inhibitor - HER2 inhibitor Pyrotinib dimaleate For research use only.

Pyrotinib dimaleate

Synonyms: SHR-1258, BLTN, Pyrroltinib dimaleate

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 Chemical Structure

Pyrotinib dimaleate Chemical Structure

CAS No. 1397922-61-0

Purity & Quality Control

Pyrotinib dimaleate Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Biological Activity

Description 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.
Targets
EGFR [1]
(Cell-free assay)		 HER2 [1]
(Cell-free assay)
0.013 μM 0.038 μM
In vitro
In vitro

Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.[1]
Cell Research Cell lines A431, SK-BR-3, NCI-N87
Concentrations 6-7 concentrations (not specific)
Incubation Time 72 h
Method

Cells are incubated in a carbon dioxide (5%CO2) incubator until they reached 85% confluency, subsequently, cell culture medium is replaced by fresh one with Pyrotinib (SHR1258) added in a series of concentrations (6 to 7 concentrations). The cells are then put back to the incubator and cultured continuously. After 72 hours, the activity of the test compounds for inhibiting the cell proliferation is determined by a sulforhodamine B (SRB) method.
In Vivo
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.[1]
Animal Research Animal Models 6-7-week-old female BALB/Ca-nude mice with BT-474/SK-OV-3 xenografts
Dosages 2.5-20 mg/kg, 100 mg/kg
Administration IV, IG
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

Chemical Information & Solubility

Molecular Weight 815.22 Formula

C40H39ClN6O11
CAS No. 1397922-61-0 SDF --
Smiles CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CC5CCCN5C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (122.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 16 mg/mL


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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.
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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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