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RET V804M-IN-1

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Chemical Structure| 2414909-94-5 同义名 : -
CAS号 : 2414909-94-5
货号 : A1275491
分子式 : C19H16N6O
纯度 : 98%+
分子量 : 344.37
MDL号 : MFCD32693930
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(348.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 RET is a single-pass transmembrane protein with a typical intracellular tyrosine kinase domain. Among the various oncogene drivers in NSCLC (non-small-cell lung cancer), the RET gene is involved in various chromosomal rearrangements, which can be found in 1%–2% of all NSCLC patients[2]. RETV804M kinase inhibitor is a wt-RET-selective inhibitor of RETV804M kinase with an IC50 of 20 nM, which exhibits 3.7 and 110 fold selectivity over wt-RET and KDR, respectively[1].
作用机制 The pyrazolopyrimidine core of RETV804M kinase inhibitor would bind to the hinge region, directing the benzamide towards the catalytic lysine (Lys758) and placing the pyridine in the pocket normally occupied by the ribose moiety of ATP[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.52mL

2.90mL

1.45mL

29.04mL

5.81mL

2.90mL
参考文献

[1]Newton R, et al. Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase. ACS Med Chem Lett. 2020 Feb 28;11(4):497-505

[2]Bronte G, et al. Targeting RET-rearranged non-small-cell lung cancer: future prospects. Lung Cancer (Auckl). 2019 Mar 20;10:27-36