MS67|cas:2407452-77-9|西域试剂

MS67,98.73%

产品编号：Bellancom-141796| CAS NO：2407452-77-9| 分子式：C₅₂H₅₉F₄N₉O₇S| 分子量：1030.14

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-141796		￥7200.00	杭州北京（现货）
Bellancom-141796		￥11500.00	杭州北京（现货）

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MS67

产品介绍

MS67 是一种有效的选择性 WD40 重复域蛋白 5 (WDR5) 降解剂，K_d 为 63 nM。MS67 对其他蛋白质甲基转移酶、激酶、GPCR、离子通道和转运蛋白无活性。MS67 显示出有效的抗癌作用。

生物活性

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a K_d of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.

体外研究

MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells.
MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin.
The GI₅₀ values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67.
. MS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a K_d of 140 nM.

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

Western Blot Analysis

Cell Line:	MV4;11 cells
Concentration:	0.001 μM, 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM
Incubation Time:	18 hours
Result:	Induced WDR5 degradation at a concentration as low as 1 nM with DC₅₀ of 3.7 nM.

体内研究
(In Vivo)

MS67 (75 mg/kg; i.p.; twice daily; 5 days a week; for 20 days) significantly inhibits tumor growth in vivo and prolongs survival of the treated mice.
After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours.

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

Animal Model:	MV4;11 MLL-r AML xenograft mouse
Dosage:	75 mg/kg
Administration:	i.p.; twice daily; 5 days a week; for 20 days
Result:	Inhibited tumor growth in vivo.

体内研究

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

Animal Model:	MV4;11 MLL-r AML xenograft mouse
Dosage:	75 mg/kg
Administration:	i.p.; twice daily; 5 days a week; for 20 days
Result:	Inhibited tumor growth in vivo.

体内研究

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

Animal Model:	MV4;11 MLL-r AML xenograft mouse
Dosage:	75 mg/kg
Administration:	i.p.; twice daily; 5 days a week; for 20 days
Result:	Inhibited tumor growth in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (97.07 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9707 mL	4.8537 mL	9.7074 mL
5 mM	0.1941 mL	0.9707 mL	1.9415 mL
10 mM	0.0971 mL	0.4854 mL	0.9707 mL

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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

参考文献