M-1211|cas:2377337-93-2|西域试剂

M-1211,99.28%

产品编号：Bellancom-132234| CAS NO：2377337-93-2| 分子式：C₄₂H₅₇FN₆O₆S| 分子量：793.00

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-132234		￥11800.00	杭州北京（现货）

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M-1211

产品介绍

M-1121 是共价并具有口服活性的 menin-MLL 相互作用抑制剂，能够实现完全和持久的肿瘤消退。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

Cell Line:	MV4;11 cells
Concentration:	0~100 nM
Incubation Time:	24 hours
Result:	Drived dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.