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

Pyrotinib dimaleate (Synonyms: SHR-1258 dimaleate)

Cat. No.: HY-104065B Purity: 98.60%
Handling Instructions

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s 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
10 mM * 1 mL in Water USD 1022 In-stock
Estimated Time of Arrival: December 31
1 mg USD 228 In-stock
Estimated Time of Arrival: December 31
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3540 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Pyrotinib dimaleate:

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  • Biological Activity

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  • Purity & Documentation

  • References

Description

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.

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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 106 mg/mL (130.03 mM)

*"≥" 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
10 mM 0.1227 mL 0.6133 mL 1.2267 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

815.22

Formula

C₄₀H₃₉ClN₆O₁₁

CAS No.

1397922-61-0

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/[[email protected]@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

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Product Name:
Pyrotinib dimaleate
Cat. No.:
HY-104065B
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Pyrotinib dimaleate

Cat. No.: HY-104065B