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  4. Menin-MLL inhibitor-22

Menin-MLL inhibitor-22 

目录号: HY-151595 纯度: 99.85%
COA 产品使用指南

摩尔计算器

Menin-MLL inhibitor-22 (compound C20) 是一种口服有效的针对 menin 和混合谱系白血病 (MLL) 相互作用的抑制剂 (IC50=7 nM)。Menin-MLL inhibitor-22 通过结合 menin 蛋白，抑制癌细胞生长 (MV4 细胞，IC50=0.3 μM)。Menin 是一种与多内分泌肿瘤 1 型 (MEN-1 综合征) 相关的肿瘤抑制因子。

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Menin-MLL inhibitor-22 Chemical Structure

Menin-MLL inhibitor-22 Chemical Structure

CAS No. : 2851841-61-5

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1 mg ￥1250
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5 mg ￥3123
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10 mg ￥4995
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Customer Review

Menin-MLL inhibitor-22 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HL-60 IC50
> 10 μM
Compound: C20
Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
[PMID: 36173787]
MV4-11 IC50
0.3 μM
Compound: C20
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
[PMID: 36173787]
MV4-11 IC50
0.3 μM
Compound: C20
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay
[PMID: 36173787]
MV4-11 IC50
0.36 μM
Compound: C20
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay
[PMID: 36173787]
体外研究
(In Vitro)

Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes[1].
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[1].
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[1].
Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest[1].

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

Menin-MLL inhibitor-22 相关抗体:

RT-PCR[1]

Cell Line: MLL-r Leukemia cells MV4;11
Concentration: 0.1, 1, and 10 μM
Incubation Time: 24 hours
Result: Reversed the over-expressing HOXA9 and MEIS1 induced by menin-MLL interaction, decreased the level of HOXA9 and MEIS1.

Apoptosis Analysis[1]

Cell Line: MLL-r Leukemia cells MV4;11
Concentration: 1, and 10 μM
Incubation Time: 24 hours
Result: Decreased in the population of cells in the S and G2/M phases, arrested cell cycle at G0/G1 phase.
体内研究
(In Vivo)

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[1].

Pharmacokinetic Properties in SD Rats[1]

Route Dose (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. 5 N/A 17.5 7.1 1187 1700 2495 2056 49.3
p.o. 15 7.3 15.5 12.0 56.7 863.7 1476 10730 23 16.9

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

Animal Model: Balb/C nude mice bearing MV4;11 cell xenografts[1]
Dosage: 6 mg/kg, 30 mg/kg
Administration: Oral gavage; every second day for 16 days
Result: Reduced the volume of tumor in mice.
分子量

565.73

Formula

C29H39N7O3S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (220.95 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7676 mL 8.8381 mL 17.6763 mL
5 mM 0.3535 mL 1.7676 mL 3.5353 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Menin-MLL inhibitor-22 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7676 mL 8.8381 mL 17.6763 mL 44.1907 mL
5 mM 0.3535 mL 1.7676 mL 3.5353 mL 8.8381 mL
10 mM 0.1768 mL 0.8838 mL 1.7676 mL 4.4191 mL
15 mM 0.1178 mL 0.5892 mL 1.1784 mL 2.9460 mL
20 mM 0.0884 mL 0.4419 mL 0.8838 mL 2.2095 mL
25 mM 0.0707 mL 0.3535 mL 0.7071 mL 1.7676 mL
30 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4730 mL
40 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1048 mL
50 mM 0.0354 mL 0.1768 mL 0.3535 mL 0.8838 mL
60 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
80 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
100 mM 0.0177 mL 0.0884 mL 0.1768 mL 0.4419 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.

Keywords:

Menin-MLL inhibitor-222851841-61-5Epigenetic Reader Domainmultiple endocrine neoplasia type 1MEN-1 syndrometumor suppressorInhibitorinhibitorinhibit

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