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

Pyrotinib dimaleate  (Synonyms: SHR-1258 dimaleate)

Cat. No.: HY-104065B Purity: 98.56%
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Pyrotinib dimaleate (SHR-1258 dimaleate) est un double inhibiteur de EGFR/HER2 qui est puissant et sélectif avec des IC50s de 13 et 38 nM, respectivement.

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.

Pyrotinib dimaleate Chemical Structure

Pyrotinib dimaleate Chemical Structure

CAS No. : 1397922-61-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 789 In-stock
Solution
10 mM * 1 mL in DMSO USD 789 In-stock
Solid
1 mg USD 190 In-stock
5 mg USD 580 In-stock
10 mg USD 880 In-stock
25 mg USD 1700 In-stock
50 mg USD 2700 In-stock
100 mg   Get quote  
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This product is a controlled substance and not for sale in your territory.

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Based on 12 publication(s) in Google Scholar

Other Forms of Pyrotinib dimaleate:

Pyrotinib dimaleate Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1]

HER2

38 nM (IC50)

EGFR

13 nM (IC50)

In Vitro

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.

Pyrotinib dimaleate Related Antibodies
In Vivo

Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t1/2=15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t1/2=1.56 h; i.g.; t1/2=2.52 h) and rat (i.v.; t1/2=4.42 h; i.g.; t1/2=3.38 h)[1].

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

815.22

Formula

C40H39ClN6O11
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.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2267 mL 6.1333 mL 12.2666 mL
5 mM 0.2453 mL 1.2267 mL 2.4533 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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].

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, 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
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.

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Pyrotinib dimaleate 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:

Pyrotinib dimaleate1397922-61-0SHR-1258 dimaleateEGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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