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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $157 | In Stock | |
5 mg | $482 | In Stock | |
10 mg | $642 | In Stock | |
25 mg | $996 | In Stock | |
50 mg | $1,370 | In Stock | |
100 mg | $1,850 | In Stock | |
1 mL x 10 mM (in DMSO) | $652 | In Stock |
Description | Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent, selective dual inhibitor of EGFR and HER2, with IC50 values of 13 nM and 38 nM, respectively. |
Targets&IC50 | EGFR:13 nM, HER2:38 nM |
In vitro | Pyrotinib dimaleate exhibits potent activity in HER2-positive cell lines (BT474, SK-OV-3), yet demonstrates significantly diminished inhibitory effects on the HER2-negative cell line (MDA-MB-231). Furthermore, it shows a high degree of selectivity, akin to HKI-272, across a range of kinases including KDR, c-Kit, PDGFRβ, c-Src, and C-Met, specifically displaying an IC50 of 790 nM for c-Src and over 3000 nM for the others. Notably, it achieves inhibition of BT474 and SK-OV-3 cells with IC50 values of 5.1 and 43 nM, respectively. |
In vivo | 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 mice (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). Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5%, and 13.5% in nude mice, rats, and dogs, respectively. |
Alias | SHR-1258 dimaleate |
Molecular Weight | 815.22 |
Formula | C40H39ClN6O11 |
Cas No. | 1397922-61-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 50 mg/mL (61.33 mM) Ethanol: 40 mg/mL (49.07 mM) DMSO: 100 mg/mL (122.67 mM) | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
Ethanol/H2O/DMSO
H2O/DMSO
DMSO
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