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Pyrotinib maleate
CAS No. 1397922-61-0
Pyrotinib maleate( SHR-1258 maleate | SHR1258 maleate )
Catalog No. M11662 CAS No. 1397922-61-0
Pyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 619 | In Stock |
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| 5MG | 458 | In Stock |
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| 10MG | 610 | In Stock |
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| 25MG | 946 | In Stock |
|
| 50MG | 1274 | In Stock |
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| 100MG | 1721 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NamePyrotinib maleate
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NoteResearch use only, not for human use.
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Brief DescriptionPyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.
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DescriptionPyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively; displays high selectivity 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 >3,000 nM); exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.Breast Cancer Phase 3 Clinical.
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In VitroPyrotinib 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).
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In VivoPyrotinib 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).
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SynonymsSHR-1258 maleate | SHR1258 maleate
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PathwayAngiogenesis
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TargetEGFR
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RecptorEGFR
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Research AreaCancer
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IndicationBreast Cancer
Chemical Information
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CAS Number1397922-61-0
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Formula Weight699.161
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Molecular FormulaC36H35ClN6O7
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Purity>98% (HPLC)
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SolubilityH2O : ≥ 106 mg/mL 130.03 mM
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SMILESCCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CC5CCCN5C.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
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Chemical Name(R,E)-N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide dimaleate
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Li X, et al. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X.
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