Pyrotinib dimaleate

製品コードS8852 バッチS885203

化学情報

	Synonyms	SHR-1258, BLTN, Pyrroltinib dimaleate	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₄₀H₃₉ClN₆O₁₁
	分子量	815.22	CAS No.	1397922-61-0
Solubility (25°C)*	体外	DMSO	100 mg/mL (122.66 mM)
		Ethanol	100 mg/mL (122.66 mM)
		Water	16 mg/mL (19.62 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pyrotinib dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.
in vitro	Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.^[1]
in vivo	Pyrotinib (SHR1258) displays robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A431, SK-BR-3, NCI-N87
	濃度	6-7 concentrations (not specific)
	反応時間	72 h
	実験の流れ	Cells are incubated in a carbon dioxide (5%CO2) incubator until they reached 85% confluency, subsequently, cell culture medium is replaced by fresh one with Pyrotinib (SHR1258) added in a series of concentrations (6 to 7 concentrations). The cells are then put back to the incubator and cultured continuously. After 72 hours, the activity of the test compounds for inhibiting the cell proliferation is determined by a sulforhodamine B (SRB) method.
動物実験	動物モデル	6-7-week-old female BALB/Ca-nude mice with BT-474/SK-OV-3 xenografts
	投薬量	2.5-20 mg/kg, 100 mg/kg
	投与方法	IV, IG

参考

[1] Xin Li, et al. Eur J Pharm Sci. 2017 Dec 15;110:51-61.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Activity and mechanism of acquired resistance to tarloxotinib in HER2 mutant lung cancer: an in vitro study [ Transl Lung Cancer Res, 2021, 10(8):3659-3670]	PubMed: 34584864
UPLC-MS/MS assay for the simultaneous determination of pyrotinib and its oxidative metabolite in rat plasma: Application to a pharmacokinetic study [ Biomed Chromatogr, 2021, e5221]	PubMed: 34331710
Clinical implications of plasma ctDNA features and dynamics in gastric cancer treated with HER2-targeted therapies [ Clin Transl Med, 2020, 10(8):e254]	PubMed: 33377634

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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