RET-IN-11

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RET-IN-11 

RET-IN-11 是一种有效的选择性 RET 抑制剂，RET 和RETV804M 的 IC50s 分别为 6.20 nM 和 18.68 nM。RET-IN-11 在 LC-2/ad 细胞中显示出抗增殖和迁移活性。RET-IN-11 诱导细胞凋亡 (apoptosis)。

RET-IN-11

RET-IN-11 Chemical Structure

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生物活性

RET-IN-11 is a potent and selective RET inhibitor with IC50s of 6.20 nM, 18.68 nM for RET and RETV804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis[1].

IC50 & Target

IC50: 6.20 nM (RET); 18.68 nM (RETV804M)[1]
体外研究
(In Vitro)

RET-IN-11 (compound 20) (72 h) shows inhibition activity with an IC50 of 18.68 nM for RETV804M, and shows anti-proliferation activities in CCDC6-RET-driven LC-2/ad cells[1].
RET-IN-11 (0-200 000 nM) shows selectivity with IC50s of 6.20, 96.38, 87.57, 1421.75, >200 000, 100.17, 112.95 nM for RET, Aurora A, CSF-1R, MAP4K4, NEK2, TRKA, FLT3, respectively[1].
RET-IN-11 (500, 1000 nM) induces cell apoptosis in LC-2/ad Cells[1].
RET-IN-11 (1, 2 µM; 48 h) inhibits the migration with the wound healing percentages of 43% and 27% at 1 µM and 2 µM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: LC-2/ad Cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activities with an IC50 of 100.26 nM.

Western Blot Analysis[1]

Cell Line: RAT1 (RETC634R), NCOA4-RET/NCOA4-RETV804M/NCOA4-RETG810R transfected HEK293T cells
Concentration: 100, 500, 2500 nM
Incubation Time: 2 h
Result: Significantly inhibits the auto-phosphorylation of RETC634R and NCOA4-RET on Y905 and Y1062 at 100 nM and 500 nM.

Apoptosis Analysis[1]

Cell Line: LC-2/ad Cells
Concentration: 500, 1000 nM
Incubation Time: 48 h
Result: Increased the fraction of apoptotic cell for 500 nM (31% increase) and 1 µM (36% increase), respectively.

分子量

515.59

Formula

C27H30FN9O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang L, et al. Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. J Med Chem. 2022 Jan 27;65(2):1536-1551.

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