Pyrotinib dimaleate
Based on 18 publication(s) in Google Scholar
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 98.04%
- CAS No.: 1397922-61-0
- Formula: C40H39ClN6O11
- Molecular Weight:815.22
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Pyrotinib dimaleate
More- Nat Cancer. 2025 Jul;6(7):1202-1222. [Abstract]
- J Thorac Oncol. 2024 Jan;19(1):106-118. [Abstract]
- J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Int J Biol Macromol. 2023 Jul 1;242(Pt 2):124870. [Abstract]
- J Med Chem. 2019 May 9;62(9):4772-4778. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Lung Cancer. 2018 Dec:126:72-79. [Abstract]
- Int J Cancer. 2024 Jul 15;155(2):324-338. [Abstract]
- iScience. 2024 Jan 9;27(2):108839. [Abstract]
- Biosci Rep. 2020 Feb 28;40(2):BSR20194167. [Abstract]
- Clin Transl Oncol. 2024 Dec;26(12):3050-3057. [Abstract]
- Open Life Sci. 2023 Jan 10;18(1):20220535. [Abstract]
- STAR Protoc. 2024 Apr 16;5(2):102987. [Abstract]
- Patent. US20250312348A1.
- Biomed Pharmacother. 2024 Nov:180:117523. [Abstract]
- Patent. US20220175778A1.
- Patent. US20210361655A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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IHC
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Cell Imaging/Staining
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Apoptosis Analysis
All EGFR Isoforms
More
Biological Activity
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HER2 38 nM (IC50) |
EGFR 13 nM (IC50) |
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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1397922-61-0
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Appearance Solid
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Molecular Weight 815.22
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Formula C40H39ClN6O11
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Color Light yellow to yellow
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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
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Synonyms
SHR-1258 dimaleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (18)
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Journal Impact Factor
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Most Recent
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Nat Cancer
p95HER2, a truncated form of the HER2 oncoprotein, drives an immunosuppressive program in HER2+ breast cancer that limits trastuzumab deruxtecan efficacy. [Abstract]2025 Jul;6(7):1202-1222. PMID: 40579589 -
J Thorac Oncol
HER4 and EGFR activate cell signaling in NRG1 fusion-driven cancers: implications for HER2/HER3-specific vs. pan-HER targeting strategies. [Abstract]2024 Jan;19(1):106-118. PMID: 37678511 -
J Exp Clin Cancer Res
Pyrotinib targeted EGFR/GRP78 mediated cell apoptosis in high EGFR gene copy number gastric cancer. [Abstract]2025 Aug 19;44(1):245. PMID: 40830980
Pyrotinib dimaleate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
Primary gastric cancer (GC-1 and GC-2) cells treated with Pyrotinib, Dacomitinib, Afatinib, or DMSO (control) at 1 µM concentration over 3 days, growth curves represent three independent experiments.
Pyrotinib dimaleate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
Western blotting analysis showed the cleaved caspase-9 level in GC cells treated with different dose of Pyrotinib (0.5, 1, 2 μM).
Pyrotinib dimaleate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
Representative immunohistochemical staining of Ki-67 and phosphorylated EGFR (p-EGFR) in xenograft tumor tissues excised from indicated mice treated with Pyrotinib (10 mg/kg, p.o.).
Pyrotinib dimaleate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
Representative TUNEL immunostaining (green) of apoptosis in xenograft tumor tissues excised from indicated mice treated with Pyrotinib (10 mg/kg, p.o.).
Pyrotinib dimaleate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
GC cells were harvested and stained with Annexin V-FITC and PI for apoptotic analysis with increasing concentrations of Pyrotinib (0.5, 1, 1.5, 2 μM) treatment for 48 h.
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Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Int J Biol Macromol
Branched-chain aminotransferase 1 promotes Schwann cell migration and proliferation to accelerate facial nerve regeneration through the Twist/FoxC1 and Sox2 pathways. [Abstract]2023 Jul 1;242(Pt 2):124870. PMID: 37196723 -
J Med Chem
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. [Abstract]2019 May 9;62(9):4772-4778. PMID: 30973735 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Lung Cancer
Activity of a novel HER2 inhibitor, poziotinib, for HER2 exon 20 mutations in lung cancer and mechanism of acquired resistance: An in vitro study. [Abstract]2018 Dec:126:72-79. PMID: 30527195 -
Int J Cancer
Establishment of patient-derived organoids for guiding personalized therapies in breast cancer patients. [Abstract]2024 Jul 15;155(2):324-338. PMID: 38533706 -
iScience
Profiling of ERBB receptors and downstream pathways reveals selectivity and hidden properties of ERBB4 antagonists. [Abstract]2024 Jan 9;27(2):108839. PMID: 38303712 -
Biosci Rep
2020 Feb 28;40(2):BSR20194167. PMID: 32022229 -
Clin Transl Oncol
Pyrotinib as a salvage treatment for patients with HER-2 positive advanced lung adenocarcinoma after the progression of afatinib treatment. [Abstract]2024 Dec;26(12):3050-3057. PMID: 38795256 -
Open Life Sci
Systemic investigation of inetetamab in combination with small molecules to treat HER2-overexpressing breast and gastric cancers. [Abstract]2023 Jan 10;18(1):20220535. PMID: 36694697 -
STAR Protoc
Protocol for identifying properties of ERBB receptor antagonists using the barcoded ERBBprofiler assay. [Abstract]2024 Apr 16;5(2):102987. PMID: 38635397 -
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Biomed Pharmacother
Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. [Abstract]2024 Nov:180:117523. PMID: 39405910 -
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Solvent & Solubility
H2O : ≥ 106 mg/mL (130.03 mM)
DMSO : 100 mg/mL (122.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.07 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.07 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Cancer cells (A431, SK-BR-3 and NCI-N87) are treated at a suitable concentration of Pyrotinib for 72 hours. Cell proliferation is determined by a sulforhodamine B (SRB) method. The IC50 values are calculated by the data of inhibition rates of serial concentrations of Pyrotinib dimaleate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Sprague Dawley (SD) rats (200-250g, 3 males and 3 females) are used .Test compounds (include Pyrotinib dimaleate) are administrated in both intravenous ( i.v. ; 3 mg/kg) and intragastric ( i.g. ;3 mg/kg) for rats to obtain their bioavailability. Plasma samples of nude mice is collected at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h after the IV administration [1].
Mice[1]:
In vivo efficacy studies are performed on BALB/Ca-nude mice (6 to 7 weeks, female) from SLAC. Nude mice are hypodermic inoculated BT-474 human breast cancer cell or SK-OV-3 ovarian cancer cell. After tumor grows to 150-250 mm3, mice are randomly divided into groups and dosed with Pyrotinib (2.5, 5, 10, 20 mg/kg) once daily. The volume of tumors and the weight of the mice are measured and recorded for 2-3 times per weeks[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 1.2267 mL | 6.1333 mL | 12.2666 mL | 30.6666 mL |
| 5 mM | 0.2453 mL | 1.2267 mL | 2.4533 mL | 6.1333 mL | |
| 10 mM | 0.1227 mL | 0.6133 mL | 1.2267 mL | 3.0667 mL | |
| 15 mM | 0.0818 mL | 0.4089 mL | 0.8178 mL | 2.0444 mL | |
| 20 mM | 0.0613 mL | 0.3067 mL | 0.6133 mL | 1.5333 mL | |
| 25 mM | 0.0491 mL | 0.2453 mL | 0.4907 mL | 1.2267 mL | |
| 30 mM | 0.0409 mL | 0.2044 mL | 0.4089 mL | 1.0222 mL | |
| 40 mM | 0.0307 mL | 0.1533 mL | 0.3067 mL | 0.7667 mL | |
| 50 mM | 0.0245 mL | 0.1227 mL | 0.2453 mL | 0.6133 mL | |
| 60 mM | 0.0204 mL | 0.1022 mL | 0.2044 mL | 0.5111 mL | |
| 80 mM | 0.0153 mL | 0.0767 mL | 0.1533 mL | 0.3833 mL | |
| 100 mM | 0.0123 mL | 0.0613 mL | 0.1227 mL | 0.3067 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Pyrotinib dimaleate Related Classifications
HY-104065B Related Classifications
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