Pyrotinib maleate

SKU: orb2655926

Description

Pyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively; displays high selectivity in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and c-Met (c-Src with an IC50 of 790 nM, and others >3,000 nM); exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.Breast Cancer Phase 3 Clinical.

Key Properties

• CAS Number: 1397922-61-0
• MW: 699.161
• Purity: >98% (HPLC)
• Formula: C₃₆H₃₅ClN₆O₇
• SMILES: CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CC5CCCN5C.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
• Target: EGFR
• Solubility: H2O : ≥ 106 mg/mL 130.03 mM

Bioactivity

• In Vivo:
  Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. 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).
• In Vitro:
  Pyrotinib dimaleate has high potency in HER2-dependent cell lines (BT474, SK-OV-3), while showing much weaker inhibition in the HER2 negative cell line (MDA-MB-231). Pyrotinib dimaleate inhibits BT474 and SK-OV-3 cells with IC50s of 5.1 and 43 nM, respectively. Pyrotinib dimaleate displays high selectivity as HKI-272 when tested in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and C-Met (c-Src with an IC50 of 790 nM, and others >3000 nM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SHR-1258 maleate | SHR1258 maleate

Quick Database Links

Gene Symbol

EGFR