Pyrotinib (SHR-1258) dimaleate

For research use only.

Catalog No.S8852 Synonyms: BLTN, Pyrroltinib dimaleate

3 publications

Pyrotinib (SHR-1258) dimaleate Chemical Structure

CAS No. 1397922-61-0

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.

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

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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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO Insoluble
Water Insoluble
Ethanol Insoluble

* 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 815.22
Formula

C40H39ClN6O11

CAS No. 1397922-61-0
Storage powder
in solvent
Synonyms 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

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

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04850651 Not yet recruiting Drug: Pyrotinib;Fluconazole Healthy Subjects Jiangsu HengRui Medicine Co. Ltd. April 19 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
NCT04315116 Not yet recruiting Drug: pyrotinib maleate|Drug: Loperamide Healthy Participants Jiangsu HengRui Medicine Co. Ltd. March 2020 Phase 1

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID