RET-IN-11 

RET-IN-11 is a potent and selective RET inhibitor with IC₅₀s 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].

IC₅₀: 6.20 nM (RET); 18.68 nM (RET^V804M)^[1]

RET-IN-11 (compound 20) (72 h) shows inhibition activity with an IC₅₀ 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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

515.59

C₂₇H₃₀FN₉O

2764891-88-3

O=C(NC1=CC=CC(F)=C1)CC2=CC=C(NC3=NC(N4CCN(C)CC4)=CC(NC5=CC(C)=NN5)=N3)C=C2

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]