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  2. Epigenetics
  3. Epigenetic Reader Domain
  4. M-1211

M-1121 是共價并具有口服活性的 menin-MLL 相互作用抑制劑，能夠?qū)崿F(xiàn)完全和持久的腫瘤消退。

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M-1211 Chemical Structure

M-1211 Chemical Structure

CAS No. : 2377337-93-2

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥9400
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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[1].

IC50 & Target

menin-MLL interaction[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HL-60 IC50
> 10000 nM
Compound: 24; M-1121
Anti-proliferative activity against human HL-60 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human HL-60 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
K562 IC50
> 10000 nM
Compound: 24; M-1121
Anti-proliferative activity against human K562 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human K562 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
KOPN-8 IC50
110 nM
Compound: 24; M-1121
Anti-proliferative activity against human KOPN-8 cells harboring MLL/ENL fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human KOPN-8 cells harboring MLL/ENL fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
MEG-01 IC50
> 10000 nM
Compound: 24; M-1121
Anti-proliferative activity against human MEG-01 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human MEG-01 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
MOLM-13 IC50
51.5 nM
Compound: 24; M-1121
Anti-proliferative activity against human MOLM-13 cells harboring MLL/AF9 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human MOLM-13 cells harboring MLL/AF9 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
MV4-11 IC50
10.3 nM
Compound: 24; M-1121
Anti-proliferative activity against human MV4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human MV4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
RS4-11 IC50
1000 nM
Compound: 24; M-1121
Anti-proliferative activity against human RS4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human RS4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
SEM IC50
51 nM
Compound: 24; M-1121
Anti-proliferative activity against human SEM cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
Anti-proliferative activity against human SEM cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay
[PMID: 34196551]
體外研究
(In Vitro)

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[1].
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[1].

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

RT-PCR[1]

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.
體內(nèi)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%[1].
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[1].
M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution[1].

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

Animal Model: SCID mice[1]
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[1]
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[1]
Dosage: 5 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Had a low clearance and a moderate volume of distribution.
分子量

793.00

Formula

C42H57FN6O6S
CAS 號
性狀

固體

顏色

White to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 7.69 mg/mL (9.70 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.2610 mL 6.3052 mL 12.6103 mL
5 mM 0.2522 mL 1.2610 mL 2.5221 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.29%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2610 mL 6.3052 mL 12.6103 mL 31.5259 mL
5 mM 0.2522 mL 1.2610 mL 2.5221 mL 6.3052 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
M-1211
目錄號：
HY-132234
需求量：