RET-IN-19

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research[1].

Signaling Pathways >> Epigenetics >> Aurora Kinase

Signaling Pathways >> MAPK/ERK Pathway >> MAP4K

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms

EGFR:56.78 ± 4. μM (IC50)

Aurora A:0.242 ± 0. μM (IC50)

Aurora B:0.536 ± 45 μM (IC50)

MAP4K4:3.428 ± 0. μM (IC50)

RET-IN-19 (compound 59) shows growth inhibition of LC-2/ad cells which RET-CCDC6 driven, with a GI50 of 0.1067 ± 0.004 μM[1]. RET-IN-19 (3 μM) shows inhibition of LC-2/ad cells migration[1]. RET-IN-19 inhibits EGFR, Aurora A, Aurora B, Nek2, CSF-1R, MAP4K4, NIK, and RET, with IC50 values of 56.78 ± 4.94, 0.242 ± 0.036, 0.536 ± 45.12, >200, 1.65 ± 0.235, 3.428 ± 0.150, >10, and 0.0068 ± 0.0003, respectively[1].

[1]. Lakkaniga NR, et al. Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation. Eur J Med Chem. 2020 Nov 15;206:112691.