Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties.
Pack Size | Availability | Price/USD | Quantity |
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5 mg | Inquiry | $ 970.00 |
Description | RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties. |
Targets&IC50 | RET (V804M):1.97 nM (IC50), RET (M918T):0.99 nM (IC50), RET (WT):1.29 nM (IC50) |
In vitro | RET-IN-4 (compound 9) effectively inhibits the proliferation of Ba/F3 cells transformed by the NSCLC-associated KIF5B-RET fusion, with an IC50 value of 19 nM. Compared to BLU-667[1], RET-IN-4 demonstrates fewer 'off-target' effects. |
In vivo | RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) effectively suppresses KIF5B-RET-Ba/F3 cell-induced tumor growth in a dose-dependent manner in immunodeficient nude/nude mice models bearing KIF5B-RET Ba/F3 cells[1]. Administration of 10-20 mg/kg of RET-IN-4 orally, once daily for a ten-day period, demonstrated significant tumor growth inhibition[1]. |
Molecular Weight | 546.611 |
Formula | C27H31FN10O2 |
CAS No. | 2436473-55-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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RET-IN-4 2436473-55-9 RETIN4 RET IN 4 inhibitor inhibit