产品
编 号：F756365
分子式：C29H39N7O3S
分子量：565.73
分子式：C29H39N7O3S
分子量：565.73
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2851841-61-5
产品详情
生物活性：
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome).
体内研究：
Menin-MLL inhibitor-22 (6 mg/kg and 30 mg/kg; p.o.; every second day for 16 days) shows potent antitumor activity in the MV4;11 subcutaneous xenograft models of MLL-rearranged leukemia.Pharmacokinetic Properties in SD RatsRouteDose (mg/kg)Tmax (h)T1/2 (h)MRT (h)Cmax (ng/mL)AUC0-t (ng·h/mL)AUC0-∞ (ng·h/mL)Cltotal (mL/h/kg)Vss (L/kg)F (%)
i.v.5N/A17.57.1118717002495205649.3
p.o.157.315.512.056.7863.71476107302316.9
Animal Model:Balb/C nude mice bearing MV4;11 cell xenografts
Dosage:6 mg/kg, 30 mg/kg
Administration:Oral gavage; every second day for 16 days
Result:Reduced the volume of tumor in mice.
体外研究：
Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes.Menin-MLL inhibitor-22 (1 and 10 μM; 24 h) inhibits MLL-r Leukemia cells MV4;11 growth and (0.1-10 μM; 24 h) decreases the expression of the HOXA9 and MEIS1 induced by menin-MLL interaction. Menin-MLL inhibitor-22 (1, and 10 μM; 7 d) increases the amount of CD11b, a differentiation marker of myeloid cells, indicating a reverse the differentiation arrest of MLL-r leukemia cells.Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest.
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome).
体内研究：
Menin-MLL inhibitor-22 (6 mg/kg and 30 mg/kg; p.o.; every second day for 16 days) shows potent antitumor activity in the MV4;11 subcutaneous xenograft models of MLL-rearranged leukemia.Pharmacokinetic Properties in SD RatsRouteDose (mg/kg)Tmax (h)T1/2 (h)MRT (h)Cmax (ng/mL)AUC0-t (ng·h/mL)AUC0-∞ (ng·h/mL)Cltotal (mL/h/kg)Vss (L/kg)F (%)
i.v.5N/A17.57.1118717002495205649.3
p.o.157.315.512.056.7863.71476107302316.9
Animal Model:Balb/C nude mice bearing MV4;11 cell xenografts
Dosage:6 mg/kg, 30 mg/kg
Administration:Oral gavage; every second day for 16 days
Result:Reduced the volume of tumor in mice.
体外研究：
Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes.Menin-MLL inhibitor-22 (1 and 10 μM; 24 h) inhibits MLL-r Leukemia cells MV4;11 growth and (0.1-10 μM; 24 h) decreases the expression of the HOXA9 and MEIS1 induced by menin-MLL interaction. Menin-MLL inhibitor-22 (1, and 10 μM; 7 d) increases the amount of CD11b, a differentiation marker of myeloid cells, indicating a reverse the differentiation arrest of MLL-r leukemia cells.Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest.
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