MRTX-1719

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Chemical Structure| 2630904-45-7 同义名 : -
CAS号 : 2630904-45-7
货号 : A1540351
分子式 : C23H18ClFN6O2
纯度 : 98%
分子量 : 464.88
MDL号 : N/A
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 MRTX-1719 is a highly potent, orally bioavailable, and selective inhibitor of the PRMT5•MTA complex, exhibiting IC50 values of 3.6 nM and 20.5 nM for PRMT5•MTA and PRMT5, respectively. It binds tightly to the PRMT5•MTA complex, with a KD value of 0.14 pM. MRTX-1719 demonstrates antineoplastic activity both in vitro and in vivo, making it a valuable tool for cancer research [1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.51mL

4.30mL

2.15mL
参考文献

[1]1. Lars D Engstrom, et al. MRTX1719 is an MTA-cooperative PRMT5 inhibitor that exhibits synthetic lethality in preclinical models and patients with MTAP deleted cancer. Cancer Discov. 2023 Aug 8;CD-23-0669.

[2]Christopher R Smith, et al. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers. J Med Chem. 2022 Feb 10;65(3):1749-1766.