| Identification | Back Directory | [Name]
4-Pyrimidinamine, 2-[6-[6-[[6-(4-fluoro-1H-pyrazol-1-yl)-3-pyridinyl]methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]-6-methyl-N-(5-methyl-1H-pyrazol-3-yl)- | [CAS]
2479961-46-9 | [Synonyms]
RET-IN-23
4-Pyrimidinamine, 2-[6-[6-[[6-(4-fluoro-1H-pyrazol-1-yl)-3-pyridinyl]methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]-6-methyl-N-(5-methyl-1H-pyrazol-3-yl)- | [Molecular Formula]
C28H28FN11 | [MOL File]
2479961-46-9.mol | [Molecular Weight]
537.59 |
| Hazard Information | Back Directory | [Uses]
RET-IN-23 (compound 17) is a potent and orally active RET inhibitor with IC50 values of 1.32, 2.50, 6.54, 1.03, 1.47 nM for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, RET-M918T, respectively. RET-IN-23 shows anti-tumor activity[1]. | [in vivo]
RET-IN-23 (5 mg/kg; p.o.) shows anti-tumor activity in mice[1]. | Animal Model: | Balb/c-nu mouse (TT cell subcutaneous xenograft tumor)[1] | | Dosage: | 5 mg/kg | | Administration: | P.o. | | Result: | Showed anti-tumor activity with T/C of 17.44%, TGI of 88.82%. |
| [References]
[1] ZhongHui Chen, et al. Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof. WO2020168939A1. |
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