| Bioactivity | 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]. |
| Target | IC50: 6.20 nM (RET); 18.68 nM (RETV804M) |
| Invitro | 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]. Cell Proliferation Assay[1] Cell Line: |
| Name | RET-IN-11 |
| Formula | C27H30FN9O |
| Molar Mass | 515.59 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |