2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Pyrotinib

Pyrotinib  (Synonyms: SHR-1258)

Cat. No.: HY-104065 Purity: 99.89%
SDS COA Handling Instructions

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Pyrotinib (SHR-1258) est un double inhibiteur de EGFR/HER2 qui est puissant et sélectif avec des IC50s de 13 et 38 nM, respectivement.

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.

Pyrotinib Chemical Structure

Pyrotinib Chemical Structure

CAS No. : 1269662-73-8

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1 mg USD 228 In-stock
5 mg USD 780 In-stock
10 mg USD 1140 In-stock
25 mg USD 2340 In-stock
50 mg USD 3540 In-stock
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Based on 15 publication(s) in Google Scholar

Other Forms of Pyrotinib:

Pyrotinib Related Antibodies

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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
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]
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.

Pyrotinib Related Antibodies
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.
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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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%

SDS (393 KB)

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

Handling Instructions (2659 KB)
References
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

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.

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
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
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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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