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Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。

RET-IN-11 is a potent and selective RET inhibitor with IC 50 s of 6.20 nM, 18.68 nM for RET and RET V804M, 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].

RET-IN-11 (compound 20) (72 h) shows inhibition activity with an IC 50 of 18.68 nM for RET V804M, and shows anti-proliferation activities in CCDC6-RET-driven LC-2/ad cells [1]. RET-IN-11 (0-200 000 nM) shows selectivity with IC 50 s 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]. Cell Proliferation Assay [1] Cell Line: LC-2/ad Cells Concentration: Incubation Time: 72 h Result: Showed anti-proliferation activities with an IC 50 of 100.26 nM. Western Blot Analysis [1] Cell Line: RAT1 (RET C634R ), NCOA4-RET/NCOA4-RET V804M /NCOA4-RET G810R transfected HEK293T cells Concentration: 100, 500, 2500 nM Incubation Time: 2 h Result: Significantly inhibits the auto-phosphorylation of RET C634R 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.

C27H30FN9O

515.59

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