产品
编 号：F751720
分子式：C42H57FN6O6S
分子量：793
分子式：C42H57FN6O6S
分子量：793
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2377337-93-2
产品详情
生物活性：
M?1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
体内研究：
M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm3 at the beginning of the treatment to 106 mm3 on day 26 of the treatment, a reduction of tumor volume of 32%.M-1121 (300 mg/kg; p.o.) leads to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment.M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution.Animal Model:SCID mice
Dosage:100 mg/kg
Administration:P.o.
Result:Reduced the average tumor volume from 157 mm3 at the beginning of the treatment to 106 mm3 on day 26 of the treatment, a reduction of tumor volume of 32%.
Animal Model:SCID mice
Dosage:300 mg/kg
Administration:P.o.
Result:Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment.
Animal Model:Female C57BL/6 mice
Dosage:5 mg/kg (Pharmacokinetic Analysis)
Administration:P.o.
Result:Had a low clearance and a moderate volume of distribution.
体外研究：
M-1121 (0~100 nM; 24 hours; MV4;11 cells) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line.M-1121 establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL.
M?1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
体内研究：
M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm3 at the beginning of the treatment to 106 mm3 on day 26 of the treatment, a reduction of tumor volume of 32%.M-1121 (300 mg/kg; p.o.) leads to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment.M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution.Animal Model:SCID mice
Dosage:100 mg/kg
Administration:P.o.
Result:Reduced the average tumor volume from 157 mm3 at the beginning of the treatment to 106 mm3 on day 26 of the treatment, a reduction of tumor volume of 32%.
Animal Model:SCID mice
Dosage:300 mg/kg
Administration:P.o.
Result:Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment.
Animal Model:Female C57BL/6 mice
Dosage:5 mg/kg (Pharmacokinetic Analysis)
Administration:P.o.
Result:Had a low clearance and a moderate volume of distribution.
体外研究：
M-1121 (0~100 nM; 24 hours; MV4;11 cells) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line.M-1121 establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL.
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