| 生物活性 | FLT3/TrKA-IN-1 is a potentFLT3/TrKAdual kinase inhibitor with theIC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM forFLT3, FLT3-ITD, FLT3-TKD andTrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well asapoptosisand shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML)[1]. |
体外研究
(In Vitro) | FLT3/TrKA-IN-1 (compound 4ACP) (1000, 2000, 3000, 4000, 5000 nM; 24, 48, 72 h) shows antiproliferative activity in a concentration and time-dependent pattera with IC50s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively[1].
FLT3/TrKA-IN-1 (500, 1000, 1500, 2000, 2500 nM) dose not elicit cytotoxic activity against GDM-1 and THP-1 AML cell lines which do not carry FLT3-ITD mutation[1].
FLT3/TrKA-IN-1 shows potent activity against colon cancer KM12 cell line with an GI50value of 358 nM[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 24 h, 48 h) inhibits ERK1/2 (extracellular regulated kinases 1/2) and mTOR (mammalian target of rapamycin) in FLT3-ITD positive AML (acute myeloid leukemia) cell lines in a dose-dependent manner[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 72 h) induces cell cycle arrest at the G0/G1 phase as well as apoptosis and necrotic cell death of FLT3-ITD harboring AML cells[1].
FLT3/TrKA-IN-1 ( 0, 1, 10, 100, 1000 nM; 72 h) dose not elicit drastic cytotoxic effects on BNL and H9c2 cells[1].
Cell Proliferation Assay[1] | Cell Line: | MV4-11, MOLM-13 cells | | Concentration: | 1000, 2000, 3000, 4000, 5000 nM | | Incubation Time: | 24, 48, 72 h | | Result: | Showed antiproliferative activity in a concentration and time-dependent pattera with IC50s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | MV4-11, MOLM-13 cells | | Concentration: | 0, 10, 50, 100 nM | | Incubation Time: | 72 h | | Result: | Induced cell cycle arrest at the G0/G1 phase. |
Apoptosis Analysis[1] | Cell Line: | MV4-11, MOLM-13 cells | | Concentration: | 0, 10, 50, 100 nM | | Incubation Time: | 72 h | | Result: | Induced apoptosis and necrotic cell death of FLT3-ITD harboring AML cells. |
Cell Cytotoxicity Assay[1] | Cell Line: | BNL, H9c2 cells | | Concentration: | 0, 1, 10, 100, 1000 nM | | Incubation Time: | 72 h | | Result: | Did not elicit drastic cytotoxic effects on BNL and H9c2 cells. |
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