Oritinib|2035089-28-0|(SH-1028)-陌孚医药/Medlife

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Oritinib (Synonyms: SH-1028)

目录号: PL03887 纯度: ≥99%

SH-1028 是一种不可逆的第三代 EGFR TKI，可克服 T790M 介导的非小细胞肺癌耐药。SH-1028 是 EGFR 激酶活性的突变选择性抑制剂，抑制 EGFR^WT、EGFR^L858R、EGFR^L861Q、EGFR^L858R/T790M、EGFR^d746-750 和

CAS No. :2035089-28-0

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中文名称	Oritinib
英文名称	Oritinib
英文别名	Oritinib
Cas No.	2035089-28-0
分子式	C₃₁H₃₇N₇O₂
分子量	539.67
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

SH-1028 是一种不可逆的第三代 EGFR TKI，可克服 T790M 介导的非小细胞肺癌耐药。SH-1028 是 EGFR 激酶活性的突变选择性抑制剂，抑制 EGFR^WT、EGFR^L858R、EGFR^L861Q、EGFR^L858R/T790M、EGFR^d746-750 和生物活性

Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR, EGFR, EGFR, EGFR, EGFR and EGFR kinases, with IC 50 s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.

性状

Solid

IC50 & Target[1][2]

EGFR (WT) 18 nM (IC50) EGFR 0.7 nM (IC

体外研究(In Vitro)

Oritinib (SH-1028) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation.
Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro.
Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h. has not independently confirmed the accuracy of these methods. They are for reference only. <

体内研究(In Vivo)

Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models.
Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues. 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

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Luwei Han, et al. SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer. Front Pharmacol. 2021 Apr 27;12:665253.

溶解度数据	In Vitro: DMSO : 125 mg/mL (231.62 mM; Need ultrasonic)配制储备液

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Data Sheet

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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。

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