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Pyrotinib dimaleate

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively[1].

Product Specifications

CAS Number

[1397922-61-0]

Product Name Alternative

SHR-1258 dimaleate

UNSPSC

12352005

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Pyrotinib_dimaleate.html

Concentration

10mM

Purity

98.01

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : ≥ 106 mg/mL

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

Molecular Formula

C40H39ClN6O11

Molecular Weight

815.22

References & Citations

[1]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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

EGFR/ErbB1/HER1; ErbB2/HER2

Citation 01

Int J Cancer. 2024 Jul 15;155 (2) :324-338.|Open Life Sci. 2023 Jan 10;18 (1) :20220535.|Biomed Pharmacother. 2024 Nov:180:117523.|Biosci Rep. 2020 Feb 28;40 (2) :BSR20194167.|Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Clin Transl Oncol. 2024 May 25.|Int J Biol Macromol. 2023 Jul 1;242 (Pt 2) :124870.|iScience. 2024 Jan 9;27 (2) :108839.|J Exp Clin Cancer Res. 2025 Aug 19;44 (1) :245.|J Med Chem. 2019 May 9;62 (9) :4772-4778.|J Thorac Oncol. 2024 Jan;19 (1) :106-118.|Lung Cancer. 2018 Dec:126:72-79.|Mol Syst Biol. 2024 Jan;20 (1) :28-55.|Nat Cancer. 2025 Jul;6 (7) :1202-1222.|Patent. US 20220175778A1.|Patent. US20210361655A1.|Patent. US20250312348A1.|STAR Protoc. 2024 Apr 16;5 (2) :102987.

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