WF-47-JS03
目录号: PL10961 纯度: ≥99%
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中文名称
WF-47-JS03
英文名称
WF-47-JS03
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
WF-47-JS03 是一种有效的选择性 RET 激酶抑制剂,比对激酶插入域受体 (KDR) 的选择性高 500 多倍。WF-47-JS03 作用于转染 KIF5B-RET 的 Ba/F3 细胞和转染 CCDC6-RET 的 LC-2/ad 肺癌细胞,IC50 分别为 1.7 nM 和 5.3 nM。可透过血脑屏障。
生物活性
WF-47-JS03 is a potent and selective RET kinase inhibitor with IC 50 s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration.
性状
Solid
体外研究(In Vitro)
WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells and Ba/F3 wild-type cell lines with IC50s of 0.99 and 1.5 μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
WF-47-JS03 significantly inhibits tumor growth in RIE KIF5B-RET xenograft mice and is well tolerated at 1, 3, and 10 mg/kg in the 10 day study. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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
参考文献
[1]. Casey J N Mathison , et al. Efficacy and Tolerability of Pyrazolo[1,5- a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (121.44 mM; Need ultrasonic)配制储备液
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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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