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Pyrotinib dimaleate

(Synonyms: SHR-1258 dimaleate)

目录号: PL01483 纯度: ≥99%

Pyrotinib dimaleate (SHR-1258 dimaleate) 是有效、选择性的 EGFR/HER2 双重抑制剂，IC 50 值分别为 13 nM 和 38 nM。

CAS No. :1397922-61-0

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中文名称	Pyrotinib dimaleate
英文名称	Pyrotinib dimaleate
英文别名	Pyrotinib Maleate;(R,E)-N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide maleate;BCP29462;(E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide maleate;Pyrotinib dimaleate
Cas No.	1397922-61-0
分子式	C₄₀H₃₉ClN₆O₁₁
分子量	815.22
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	Pyrotinib dimaleate (SHR-1258 dimaleate) 是有效、选择性的 EGFR/HER2 双重抑制剂，IC 50 值分别为 13 nM 和 38 nM。

产品详情

Pyrotinib dimaleate (SHR-1258 dimaleate) 是有效、选择性的 EGFR/HER2 双重抑制剂，IC₅₀ 值分别为 13 nM 和 38 nM。

生物活性

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC 50 s of 13 and 38 nM, respectively.

性状

Solid

IC50 & Target[1][2]

HER2 38 nM (IC50) EGFR 13 nM (IC50

体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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; t 1/2 =15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t 1/2 =1.56 h; i.g.; t 1/2 =2.52 h) and rat (i.v.; t 1/2 =4.42 h; i.g.; t 1/2 =3.38 h). has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Li X, et al. Discovery and development of Pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X.

溶解度数据	In Vitro: H₂O : ≥ 106 mg/mL (130.03 mM)DMSO : 100 mg/mL (122.67 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Pyrotinib dimaleate

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