Pyrotinib

For research use only. Not for therapeutic Use.

  • CAT Number: I008931
  • CAS Number: 1269662-73-8
  • Molecular Formula: C32H31ClN6O3
  • Molecular Weight: 583.089
  • Purity: ≥95%
Inquiry Now

Pyrotinib (CAT: I008931), also known as SHR-1258, is a dual kinase inhibitor targeting both the epidermal growth factor receptor (EGFR or HER-1) and the human epidermal growth factor receptor 2 (ErbB2 or HER-2). It is administered orally and exhibits potential antineoplastic activity. Pyrotinib works by binding to and inhibiting the activity of EGFR and HER2, leading to the inhibition of tumor growth, angiogenesis, and regression in tumor cells expressing these receptors. EGFR and HER2 are receptor tyrosine kinases that are overexpressed in various tumor types, playing critical roles in tumor cell proliferation and the development of tumor blood vessels. Pyrotinib’s dual inhibition of EGFR and HER2 makes it a promising candidate for targeted cancer therapy.


Catalog Number I008931
CAS Number 1269662-73-8
Synonyms

Pyrotinib; SHR-1258; SHR1258; SHR 1258; Pyrotinib maleate;(R,E)-N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide

Molecular Formula C32H31ClN6O3
Purity ≥95%
Target EGFR inhibitor
Solubility Soluble in DMSO, not in water
Storage 0 - 4 °C for short term, or -20 °C for long term
Related CAS 1397922-61-0    
Overview of Clinical Research

<span style=”color:#000000;”><span style=”font-family:arial,helvetica,sans-serif;”><span style=”font-size:12px;”>Pyrotinib is an ERBB 2 receptor antagonist. The&nbsp;<span style=”font-variant-ligatures: normal; orphans: 2; widows: 2;”>Phase-III clinical trials in Non-small cell lung cancer (Late-stage disease, Second-line therapy or greater) in Belgium (PO) (EudraCT2020-000951-11) are ongoing.</span></span></span></span>

IUPAC Name (E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide
InChI InChI=1S/C32H31ClN6O3/c1-3-41-30-17-27-25(16-28(30)38-31(40)12-10-24-8-6-14-39(24)2)32(21(18-34)19-36-27)37-22-9-11-29(26(33)15-22)42-20-23-7-4-5-13-35-23/h4-5,7,9-13,15-17,19,24H,3,6,8,14,20H2,1-2H3,(H,36,37)(H,38,40)/b12-10+/t24-/m1/s1
InChIKey SADXACCFNXBCFY-IYNHSRRRSA-N
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
Reference

<br />
1:Phase I Study and Biomarker Analysis of Pyrotinib, a Novel Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor, in Patients With Human Epidermal Growth Factor Receptor 2-Positive Metastatic Breast Cancer. Ma F, Li Q, Chen S, Zhu W, Fan Y, Wang J, Luo Y, Xing P, Lan B, Li M, Yi Z, Cai R, Yuan P, Zhang P, Li Q, Xu B.J Clin Oncol. 2017 May 12:JCO2016696179. doi: 10.1200/JCO.2016.69.6179. [Epub ahead of print] PMID: 28498781<br />
2:Discovery and development of pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Li X, Yang C, Wan H, Zhang G, Feng J, Zhang L, Chen X, Zhong D, Lou L, Tao W, Zhang L.Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X. doi: 10.1016/j.ejps.2017.01.021. [Epub ahead of print] PMID: 28115222<br />
3:Metabolic characterization of pyrotinib in humans by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. Zhu Y, Li L, Zhang G, Wan H, Yang C, Diao X, Chen X, Zhang L, Zhong D.J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Oct 15;1033-1034:117-27. doi: 10.1016/j.jchromb.2016.08.009. Epub 2016 Aug 7. PMID: 27541626

Request a Quote