Pyrotinib dimaleate

SKU: orb1309199

Description

Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR and HER2, with respective IC50 values of 13 nM and 38 nM. It is a key research compound for studying HER2-positive breast cancer, demonstrating efficacy in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1397922-61-0
• MW: 815.22
• Purity: 99.52% (May vary between batches)
• Formula: C₄₀H₃₉ClN₆O₁₁
• SMILES: OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)\C=C\[C@H]1CCCN1C
• Target: HER,EGFR
• Solubility: DMSO:240 mg/mL (294.4 mM);H2O:50 mg/mL (61.33 mM);Ethanol:40 mg/mL (49.07 mM)

Bioactivity

• Target IC50:
  EGFR:13 nM|HER2:38 nM
• In Vivo:
  METHODS: Nude mice with tumor xenografts of BT-474 or SK-BR-3 cells were treated with Pyrotinib dimaleate (10 mg/kg, gavage, 21 days), chrysin (50 mg/kg), or their combination, and the effect of miR-16-5p expression level on anti-tumor efficacy was analyzed. RESULTS Combination therapy of pyrotinib dimaleate and chrysin synergistically enhanced autophagy in HER2-positive breast cancer cells by regulating the miR-16-5p/ZBTB16/G6PD axis.
• In Vitro:
  METHODS: SK-BR-3 cells were treated with Pyrotinib dimaleate (10nM) + chrysin (20μM) or drug + mimics and drug + si-ZBTB16, and the cells were collected for apoptosis analysis. RESULTS Pyrotinib dimaleate + chrysin treatment led to a significant upregulation of ZBTB16 expression, and this effect was neutralized by knockdown of ZBTB16 by siRNA-ZBTB16; miR-16-5p overexpression or ZBTB16 knockdown correspondingly reduced the apoptosis rate induced by Pyrotinib dimaleate + chrysin treatment.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HER1, HER2, Inhibitor, Epidermal growth factor receptor, EGFR, ErbB-1, inhibit, Pyrotinib Dimaleate, Pyrotinib, Pyrotinib dimaleate, SHR 1258 Dimaleate, SHR 1258, SHR-1258, SHR1258 Dimaleate, SHR-1258 dimaleate, SHR-1258 Dimaleate, SHR1258

Compound Identifiers

PubChem CID

72710866