JNJ-64619178|2086772-26-9|(JNJ-64619178)-陌孚医药/Medlife

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JNJ-64619178 (Synonyms: JNJ-64619178)

目录号: PL15063 纯度: ≥99%

CAS No. :2086772-26-9

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中文名称	JNJ-64619178
英文名称	JNJ-64619178
英文别名	A16861;(1S,2R,3S,5R)-3-[2-(2-Amino-3-bromoquinolin-7-yl)ethyl]-5-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol;JNJ-64619178;Onametostat
Cas No.	2086772-26-9
分子式	C₂₂H₂₃BrN₆O₂
分子量	483.36
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

JNJ-64619178 (Onametostat) 是一种伪不可逆的、口服活性的、选择性蛋白精氨酸甲基转移酶 5 (PRMT5) 抑制剂，IC₅₀ 为 0.14 nM。JNJ-64619178 有潜力用于肺癌的研究。

生物活性

JNJ-64619178 (Onametostat) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC 50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.

性状

Solid

IC50 & Target[1][2]

IC50: 0.14 nM (PRMT5)

体外研究(In Vitro)

JNJ-64619178 binds simultaneously to the S-adenosylmethionine (SAM)- and protein substrate- binding pockets of the PRMT5/MEP50 complex with a pseudo-irreversible mode-of-action. JNJ-64619178 shows potent and broad inhibition of cellular growth. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Oral administration of JNJ-64619178 results in efficient inhibition of dimethylation of SMD1/3 proteins, components of the splicing machinery and direct substrates of the methylosome, in several non-small cell lung cancer and small cell lung cancer cancer mouse xenograft models. 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]. Tongfei Wu, et al. Abstract 4859: JNJ-64619178, a selective and pseudo-irreversible PRMT5 inhibitor with potent in vitro and in vivo activity, demonstrated in several lung cancer models.
[2]. Tao H, et al. Discovery of Novel PRMT5 Inhibitors by Virtual Screening and Biological Evaluations. Chem Pharm Bull (Tokyo). 2019;67(4):382-388.

溶解度数据	In Vitro: DMSO : 125 mg/mL (258.61 mM; Need ultrasonic)配制储备液

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产品使用指南

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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