Pyrotinib (SHR-1258) dimaleate

Catalog No.S8852 Synonyms: BLTN, Pyrroltinib dimaleate

For research use only.

Pyrotinib (SHR-1258, BLTN, Pyrroltinib) 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 (SHR-1258) dimaleate Chemical Structure

CAS No. 1397922-61-0

Selleck's Pyrotinib (SHR-1258) dimaleate has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description Pyrotinib (SHR-1258, BLTN, Pyrroltinib) 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

Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.[1]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

DMSO Insoluble
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 815.22
Formula

C40H39ClN6O11

CAS No. 1397922-61-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CC5CCCN5C

In vivo Formulation Calculator (Clear solution)

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

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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.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04850651 Completed Drug: Pyrotinib;Fluconazole Healthy Subjects Jiangsu HengRui Medicine Co. Ltd. April 16 2021 Phase 1
NCT04680091 Active not recruiting Drug: Pyrotinib Maleate|Drug: Efavirenz Healthy Subjects Drug-drug Interaction Pyrotinib Jiangsu HengRui Medicine Co. Ltd. November 12 2020 Phase 1
NCT04447118 Recruiting Drug: Pyrotinib|Drug: Docetaxel Non-squamous NSCLC|HER2 Exon 20 Mutation Jiangsu HengRui Medicine Co. Ltd. September 11 2020 Phase 3
NCT04367090 Recruiting Drug: Docetaxel trastuzumab|Drug: Pyrotinib Metastatic Breast Cancer Jiangsu HengRui Medicine Co. Ltd. May 28 2020 Phase 1
NCT04315116 Not yet recruiting Drug: pyrotinib maleate|Drug: Loperamide Healthy Participants Jiangsu HengRui Medicine Co. Ltd. March 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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