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RET-IN-4

Catalog No. T40097Cas No. 2436473-55-9

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.

RET-IN-4

RET-IN-4

Catalog No. T40097Cas No. 2436473-55-9
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.
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Product Introduction

Bioactivity
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 (M918T):0.99 nM (IC50), RET (V804M):1.97 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].
Chemical Properties
Molecular Weight546.611
FormulaC27H31FN10O2
Cas No.2436473-55-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Keywords

RET-IN-4RETIN4RET IN 4
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