Rezivertinib|1835667-12-3|(BPI-7711)-陌孚医药/Medlife

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Rezivertinib (Synonyms: BPI-7711)

目录号: PL01785 纯度: ≥99%

CAS No. :1835667-12-3

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中文名称	Rezivertinib
英文名称	Rezivertinib
英文别名	Rezivertinib;2-enamide;U65F5M6BD5;methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-;N-(2-[2-(dimethylamino)ethoxy]-4-methoxy-5-{[4-(1-;Rezivertinib [INN];GTPL10628;example 1 [WO2016094821A2];CN(CCOC1=C(C=C(C(=C1)OC)NC1=NC=CC(=N1)C1=CN(C2=CC=CC=C12)C)NC(C=C)=O)C;2-Propenamide, N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-;N-(2-(2-(Dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-
Cas No.	1835667-12-3
分子式	C₂₇H₃₀N₆O₃
分子量	486.57
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Rezivertinib (BPI-7711) 是一种口服有效，高选择性和不可逆的第三代 EGFR 酪氨酸激酶抑制剂 (TKI)。Rezivertinib 对常见的激活 EGFR 和抗性T790M 突变具有高效力。Rezivertinib 具有出色的透过中枢神经系统 (CNS) 能力，并具有抗肿瘤活性。

生物活性

Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.

性状

Solid

IC50 & Target[1][2]

EGFR

体外研究(In Vitro)

Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT).
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression.
Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model.
Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days).
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]. Misako Nagasaka, et al. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763.
[2]. Victoria L. Wilde, et al. Preclinical evidence of BPL-7711 activity in Egfr-mutant non-smallcell lung cancer ( NSCLC ) in orthotopically implanted human tumorxenografts in the lung and brain.

溶解度数据	In Vitro: DMSO : 125 mg/mL (256.90 mM; Need ultrasonic)配制储备液

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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。

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