XMU-MP-3|cas:2031152-08-4|西域试剂

XMU-MP-3,98.27%

产品编号：Bellancom-136531| CAS NO：2031152-08-4| 分子式：C₂₇H₂₇F₃N₈O| 分子量：536.55

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-136531	￥4500.00	杭州北京（现货）
Bellancom-136531	￥7800.00	杭州北京（现货）
Bellancom-136531	￥23000.00	杭州北京（现货）
Bellancom-136531	￥36000.00	杭州北京（现货）

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XMU-MP-3

产品介绍

XMU-MP-3 是一种有效的非共价 BTK 抑制剂，在 10 μM ATP 存在下，对 BTK WT 和 BTK C481S 突变型的 IC₅₀ 分别为 10.7 nM 和 17.0 nM。XMU-MP-3 也诱导凋亡 (apoptosis)。

生物活性

XMU-MP-3 is a potent non-covalent BTK inhibitor with IC₅₀s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.

体外研究

XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC₅₀ of 11.4 nM.
XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC₅₀ values of 326.6 nM, 685.6 nM and 1065 nM, respectively.
XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC₅₀ of 182.3 nM against BTK(C481S)-Ba/F3 cells.
XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells.
XMU-MP-3 (10-1000 nM; 4 hours) inhibits both the auto- and trans-phosphorylation of BTK at the site of Y223 and Y551 in a dose-dependent manner in BTK-transformed Ba/F3 cells.

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

Cell Proliferation Assay

Cell Line:	BTK-transformed and parental Ba/F3 cells
Concentration:	0.001, 0.01, 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:	48 hours
Result:	Inhibited BTK-transformed Ba/F3 cell proliferation with an IC₅₀ of 11.4 nM, while it showed negligible anti-proliferative effects on parental wild-type Ba/F3 cells (IC₅₀ >10000 nM).

Western Blot Analysis

Cell Line:	BTK-transformed Ba/F3 cells
Concentration:	10, 50, 100, 500, 1000 nM
Incubation Time:	4 hours
Result:	The phosphorylation levels of BTK Y223 and Y551 were reduced significantly at concentrations as low as 100 nM, and completely suppressed at the concentration of 1000 nM.

体内研究
(In Vivo)

XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models.

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

Animal Model:	Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models
Dosage:	25 and 50 mg/kg
Administration:	Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days
Result:	Significantly reduced the tumor size without affecting animal weights.

体内研究

XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models.

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

Animal Model:	Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models
Dosage:	25 and 50 mg/kg
Administration:	Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days
Result:	Significantly reduced the tumor size without affecting animal weights.

体内研究

XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models.

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

Animal Model:	Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models
Dosage:	25 and 50 mg/kg
Administration:	Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days
Result:	Significantly reduced the tumor size without affecting animal weights.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (186.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8638 mL	9.3188 mL	18.6376 mL
5 mM	0.3728 mL	1.8638 mL	3.7275 mL
10 mM	0.1864 mL	0.9319 mL	1.8638 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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。