|(1S,2R,3S,5R)-3-(2-(2-氨基-3-溴喹啉-7-基)乙基)-5-(4-氨基-7H-吡咯并[2,3-d]嘧啶-7-基)环戊烷-1,2-二醇|CsnPharm

CAS No.: 2086772-26-9

Onametostat Catalog No. CSN29543

Synonyms: Onametostat

JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer.

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400-920-2911

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技术信息

生物活性

描述Protein arginine methyltransferase 5 (PRMT5) is responsible for the mono-methylation and symmetric dimethylation of arginine, and its expression level and methyl transferring activity have been demonstrated to have a close relationship with tumorigenesis, development and poor clinical outcomes of human cancers^[1].Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties. JNJ-64619178, dosed orally (10 mg/kg, every day), shows selective and efficient blockage of the methylation of SMD1/3 proteins, which are crucial components of the spliceosome and substrates of PRMT5/MEP50. JNJ-64619178 also demonstrates tumor regression in a biomarker-driven human small cell lung cancer xenograft model (NCI-H1048) and prolongs tumor growth inhibition after dosing cessation^[2].JNJ-64619178 demonstrated a prolonged inhibition of PRMT5 and potent antiproliferative activity in subsets of cancer cell lines derived from various histologies, including lung, breast, pancreatic, and hematological malignancies^[3].
参考文献

[1] Kongkai Zhu, Jingwei Shao,et al. Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity. J Comput Aided Mol Des.2019 Aug;33(8):775-785.
[2] Dirk Brehmer,et al. Abstract DDT02-04: A novel PRMT5 inhibitor with potent in vitro and in vivo activity in preclinical lung cancer models.
[3] Dirk Brehmer, Lijs Beke,et al. Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity. Mol Cancer Ther. 2021 Dec;20(12):2317-2328.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0688 mL
- 10.3442 mL
- 20.6885 mL
- 5 mM
- 0.4138 mL
- 2.0688 mL
- 4.1377 mL
- 10 mM
- 0.2069 mL
- 1.0344 mL
- 2.0688 mL

技术信息

CAS号	2086772-26-9	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C22H23BrN6O2	运输	蓝冰
分子量	483.36	别名	Onametostat

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