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编 号：F116873
分子式：C17H21FN6O
分子量：344.39
分子式：C17H21FN6O
分子量：344.39
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CAS No: 1312691-33-0
产品详情
生物活性：
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
体内研究：
TAK-659 (100 mg/kg/day; p.o.; for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments. TAK-659 treatment kills tumor cells, but not host cells within the spleen and tumors.TAK-659 treatment abrogates metastasis of tumor cells into bone marrow.Animal Model:LMP2A/MYC double transgenic mice
Dosage:100 mg/kg/day
Administration:Oral gavage; for 10 days
Result:Inhibited LMP2A-induced tumor cell survival in vivo.
体外研究：
TAK-659 inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines.TAK-659 (5 μM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment.TAK-659 (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells.
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
体内研究：
TAK-659 (100 mg/kg/day; p.o.; for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments. TAK-659 treatment kills tumor cells, but not host cells within the spleen and tumors.TAK-659 treatment abrogates metastasis of tumor cells into bone marrow.Animal Model:LMP2A/MYC double transgenic mice
Dosage:100 mg/kg/day
Administration:Oral gavage; for 10 days
Result:Inhibited LMP2A-induced tumor cell survival in vivo.
体外研究：
TAK-659 inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines.TAK-659 (5 μM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment.TAK-659 (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells.
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