Pyrotinib (Synonyms: SHR-1258)

Name: Pyrotinib
Brand: MedChemExpress
SKU: HY-104065
Rating: 5.0 (18 reviews)

Cat. No.: HY-104065 Purity: 99.89%: Data Sheet
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Pyrotinib (SHR-1258) 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.

CAS No. : 1269662-73-8

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Based on 18 publication(s) in Google Scholar

Other Forms of Pyrotinib:

18 Publications Citing Use of MCE Pyrotinib

Cell Proliferation/Viability Assay

IHC

Cell Imaging/Staining

Apoptosis Analysis

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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.

Clinical Trial

Molecular Weight

583.08

Formula

C₃₂H₃₁ClN₆O₃

CAS No.

1269662-73-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (275 KB) SDS (394 KB)

COA (249 KB) HNMR (287 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Pyrotinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pyrotinib1269662-73-8SHR-1258SHR1258SHR 1258EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Pyrotinib (Synonyms: SHR-1258)

Customer Review

Other Forms of Pyrotinib:

Pyrotinib Related Antibodies

18 Publications Citing Use of MCE Pyrotinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Pyrotinib Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Pyrotinib Related Classifications

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