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编 号:F762445
分子式:C31H43ClN6O4
分子量:599.16
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10mM*1mL in DMSO
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50mg
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100mg
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生物活性:
Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.

体内研究:
Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days.Animal Model:Athymic nude mice injected with Ba/F3 cells
Dosage:60 mg/kg
Administration:Oral gavage; daily; for 35 days
Result:Caused a statistically significant increase in survival that was extended on average by 20 days.

体外研究:
Tandutinib (0-3 μM; 30 minutes; Ba/F3 cells) treatment inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10-100 nM in Ba/F3 cells expressing different FLT3-ITD mutants.Tandutinib (1 μM; 24-96 hours; Molm-14 and THP-1 AML cells) treatment induces apoptosis in FLT3-ITD-positive AML cells.In human FLT3-ITD-positive AML cell lines, Tandutinib inhibits FLT3-ITD phosphorylation (IC50 of ~30 nM). As with Erk2, a constitutively high level of Akt phosphorylation is readily detected and is efficiently blocked by pretreatment of the Molm-14 cells with 100-300 nM Tandutinib.Tandutinib inhibits cell proliferation of the FLT3-ITD-positive Molm-13 and Molm-14 with an IC50 of 10 nM. And signaling through the MAP kinase and PI3 kinase pathways.
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