Referencia número: HY-104065

Pyrotinib

(Synonyms: SHR-1258)

18 Cited Publications

Revisión del cliente

Based on 18 publication(s) in Google Scholar

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

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Pureza: 99.89%
No. CAS: 1269662-73-8
Fòrmula: C₃₂H₃₁ClN₆O₃
Peso molecular:583.08

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pyrotinib Chemical Structure

No. CAS: 1269662-73-8

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (18)
Solvente y solubilidad
- In Vitro
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

IC₅₀ & Target^[1]

EGFR

13 nM (IC₅₀)

HER2

38 nM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	15 nM Compound: Pyrotinib	Antiproliferative activity against mouse BaF3 cells harbouring HER2 A775_G77insYVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against mouse BaF3 cells harbouring HER2 A775_G77insYVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
BaF3	IC₅₀	24.67 nM Compound: Pyrotinib	Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay	[PMID: 38518121]
BT-474	IC₅₀	3.97 nM Compound: Pyrotinib	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
COLO-678	IC₅₀	1836.96 nM Compound: Pyrotinib	Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
ES-2	IC₅₀	778.34 nM Compound: Pyrotinib	Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
MDA-MB-468	IC₅₀	659.49 nM Compound: Pyrotinib	Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
MFE-280	IC₅₀	1559.06 nM Compound: Pyrotinib	Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-H441	IC₅₀	1886.34 nM Compound: Pyrotinib	Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-N87	IC₅₀	0.85 nM Compound: Pyrotinib	Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NUGC-4	IC₅₀	60.8 nM Compound: Pyrotinib	Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
SK-BR-3	IC₅₀	14 nM Compound: Pyrotinib	Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]

In Vitro

Pyrotinib 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). It inhibits BT474 and SK-OV-3Pyrotinib cells with IC₅₀s of 5.1 and 43 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pyrotinib has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. The TGI % (tumor growth inhibition) of Pyrotinib on day 21 is 109%, 157%, 159% at the doses of 5 mg/kg, 10 mg/kg, 20 mg/kg respectively. Pyrotinib in SK-OV-3 ovarian xenograft model shows TGI% on day 21 of 2%, 12%, 83% at the doses of 2.5 mg/kg, 5 mg/kg, 10 mg/kg respectively), which further confirms its robust in vivo antitumor efficacy at 10 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1269662-73-8
Appearance Solid
Peso molecular 583.08
Fòrmula C₃₂H₃₁ClN₆O₃
Color Light yellow to yellow
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
Synonyms

SHR-1258
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

All Cell Proliferation/Viability AssayWBIHCCell Imaging/StainingApoptosis Analysis

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Journal Impact Factor

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 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 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 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 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 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.
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

Radiosensitization of HER2-positive esophageal cancer cells by pyrotinib. [Abstract]

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
Patent

US20250312348A1.
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
Patent

US20220175778A1.
Patent

US20210361655A1.

Solvente y solubilidad

In Vitro:

1 M Maleic Acid : 100 mg/mL (171.50 mM; Need ultrasonic)

0.1 M Maleic Acid : 16.67 mg/mL (28.59 mM; Need ultrasonic)

DMSO : 10 mg/mL (17.15 mM; ultrasonic and adjust pH to 6 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7150 mL

8.5752 mL

17.1503 mL

5 mM

0.3430 mL

1.7150 mL

3.4301 mL

10 mM

0.1715 mL

0.8575 mL

1.7150 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Protocolo

Cell Assay^[1]

Cancer cells (A431, SK-BR-3 and NCI-N87) are treated with a series of concentrations 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 test compounds^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Rats: Test compounds (include Pyrotinib) are administrated in both intravenous (i.v.) and intragastric (i.g.) for mice 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: 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 week^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / 0.1 M Maleic Acid / 1 M Maleic Acid	1 mM	1.7150 mL	8.5752 mL	17.1503 mL	42.8758 mL
	5 mM	0.3430 mL	1.7150 mL	3.4301 mL	8.5752 mL
	10 mM	0.1715 mL	0.8575 mL	1.7150 mL	4.2876 mL
	15 mM	0.1143 mL	0.5717 mL	1.1434 mL	2.8584 mL
0.1 M Maleic Acid / 1 M Maleic Acid	20 mM	0.0858 mL	0.4288 mL	0.8575 mL	2.1438 mL
0.1 M Maleic Acid / 1 M Maleic Acid	25 mM	0.0686 mL	0.3430 mL	0.6860 mL	1.7150 mL
1 M Maleic Acid	30 mM	0.0572 mL	0.2858 mL	0.5717 mL	1.4292 mL
	40 mM	0.0429 mL	0.2144 mL	0.4288 mL	1.0719 mL
	50 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8575 mL
	60 mM	0.0286 mL	0.1429 mL	0.2858 mL	0.7146 mL
	80 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5359 mL
	100 mM	0.0172 mL	0.0858 mL	0.1715 mL	0.4288 mL

Keywords

Pyrotinib

18 Cited Publications

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Pyrotinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Pyrotinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (18)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pyrotinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Pyrotinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (18)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pyrotinib Related Classifications

HY-104065 Related Classifications