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Pyrotinib

Cat. No. M9737
Pyrotinib Structure
Synonym:

SHR-1258

Size Price Availability Quantity
2mg USD 320  USD400 In stock
5mg USD 600  USD750 In stock
10mg USD 816  USD1020 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Pyrotinib (SHR-1258) is an orally bioavailable, potent and selective EGFR/HER2 dual inhibitor, with IC50 values of 13 and 38 nM, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 583.08
Formula C32H31ClN6O3
CAS Number 1269662-73-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

[1] Xin Li, et al. Eur J Pharm Sci. Discovery and development of pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer

[2] Yunting Zhu, et al. J Chromatogr B Analyt Technol Biomed Life Sci. Metabolic characterization of pyrotinib in humans by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry

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Keywords: Pyrotinib, SHR-1258 supplier, EGFR/HER2, inhibitors

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