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Pyrotinib dimaleate Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753753

Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR/HER2 (IC50 s of 13 and 38nM, respectively). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Pyrotinib dimaleate, Inhibitor
Full Product Name
Pyrotinib dimaleate
Product Synonym Names
SHR-1258 dimaleate
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
815.22
Solubility
H2O: 106mg/mL (130.03mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C40H39ClN6O11
SMILES
O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)C2=C1)/C=C/[C@@H]5N(C)CCC5.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
CAS Number
1397922-61-0
Target & IC50
HER2: ic50 38nM
EGFR: ic50 13nM
In Vitro
Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t1/2=15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t1/2=1.56 h; i.g.; t1/2=2.52 h) and rat (i.v.; t1/2=4.42 h; i.g.; t1/2=3.38 h).Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively.

Product References and Citations for Pyrotinib dimaleate, inhibitor

Li X, et al. Discovery and development of Pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment,of breast cancer. Eur J Pharm Sci. 2017 Jan 2pii: S0928-0987(17)30043-X.
Li X, et al. Discovery and development of Pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment,of breast cancer. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X.

Other Notes

Small volumes of Pyrotinib dimaleate, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Pyrotinib dimaleate purchase

MBS5753753 is an inhibitor targeting Pyrotinib dimaleate.
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