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RET Receptor Tyrosine Kinase Inhibitor
1,3-Dihydro-5,6-dimethoxy-3-((4-hydroxyphenyl)methylene)-2H-indol-2-one, RPI-1
A cell-permeable, indolinone-based ATP-competitive tyrosine kinase inhibitor that is known to target Ret (IC50 = 170 nM), EGFR, and Met. Selectively reverts the morphologic phenotype of ret oncogene- (PTC1 & MEN2A), but not H-Ras-, transformed NIH3T3 in a reversible manner. RPI-1 effectively inhibits the autophosphorylation of PTC1, MEN2A, and Met (IC50 against Met Tyr1234/1235 in N592 ≤7.5 µM) in cancer cells, and concomitant receptor down-regulation has also been reported to occur in NIH3T3MEN2A and in small cell lung carcinoma cell line N592. Orally available in mice and is efficacious in inhibiting MEN2A- and Met-mediated tumorigenesis both in vitro (IC50 against NIH3T3MEN2A and TT proliferation = 3.6 and 7.2 µM, respectively) and in various murine xenograft models in vivo (50 to 150 mg/kg, b.i.d.).
产品信息
Form Brown solid
Molar mass 297.3
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥97% by HPLC
Solubility DMSO
Chemical formula C17H15NO4
CAS number 269730-03-2
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |