RET-IN-4 

RET-IN-4 is a potent, selective and orally active RET inhibitor with IC₅₀s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC₅₀ of 4.4 nM) and FLT3 (IC₅₀ of 30.8 nM). RET-IN-4 has anticancer effects^[1].

IC50: 1.29 nM (RET (WT)), 1.97 nM (RET (V804M)), and 0.99 nM (RET (M918T))^[1]

The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC₅₀ of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667^[1].

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

RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner^[1].

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

546.60

C₂₇H₃₁FN₁₀O₂

2436473-55-9

O=C1N([C@H](C2=CC=C(N3N=CC(F)=C3)N=C2)C)CCOC14CCN(C5=NC(NC6=NNC(C)=C6)=CC(C)=N5)CC4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhibo Luo, et al. Discovery and Optimization of Selective RET Inhibitors via Scaffold Hopping. Bioorg Med Chem Lett. 2021 May 28;128149.  [Content Brief]