2. MAPK/ERK Pathway
  3. Mixed Lineage Kinase
  4. M443

M443 是 MRK 的一个不可逆的、特异性抑制剂，其 IC50 值 <125 nM。

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M443

M443 Chemical Structure

CAS No. : 1820684-31-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5189
In-stock
1 mg ￥1600
In-stock
5 mg ￥4000
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

M443 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

M443 is an irreversible and specific inhibitor of MRK, with an IC50<125 nM.

IC50 & Target

IC50: <125 nM (MRK)[1].
体外研究
(In Vitro)

MRK 耗竭导致细胞在接受 3 Gy 辐射后存活率较对照组降低 33%。同样，克隆形成试验也显示存活率显著下降，在存活率达到 10% 时剂量增强因子 (DEF) 为 1.6。辐射后 30 分钟，MRK 激活达到峰值。因此，后续分析将以此时间点为准。在两种细胞培养中，500 nM M443 均显著抑制了 IR 刺激的 MRK、Chk2 和 p38 激活。将细胞接种于盖玻片上，用 500 nM M443 或载体预处理，接受 6 Gy 辐射照射，在辐射后不同时间固定，并用特异性染色有丝分裂细胞的 MPM2 磷酸化特异性抗体进行免疫荧光染色。与对照组细胞相比，经 M443 处理的细胞在接受 IR 后未能停滞，并保持与未接受辐射的细胞相似的有丝分裂指数。因此，抑制 MRK 会导致 Chk2 受到抑制，并且无法在响应 IR 诱导的 DNA 损伤时在细胞周期中停滞[1]。

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

M443 相关抗体:
体内研究
(In Vivo)

对照组小鼠在肿瘤细胞植入后存活时间中位数为 32 天。M443 单独治疗可使其存活时间延长 5.5 天，而所选的低剂量放射治疗并未显著提高存活时间。相比之下，M443 联合放射治疗可使存活时间中位数比对照组延长 16 天。M443 治疗不会影响动物体重，因为所有组动物在濒死前几天都观察到了体重减轻。结果表明，含肿瘤脑区的总 MRK 水平和活性 MRK 水平均升高。相反，M443 治疗组脑区的含肿瘤脑区 MRK 活性完全丧失。有趣的是，对照组脑区中含有一定水平的正常脑区 MRK 蛋白，而治疗组脑区中也失去了 MRK，这表明 M443 在整个小脑中的扩散也抑制了正常的 MRK[1]。

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

589.61

Formula

C31H30F3N7O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 55 mg/mL (93.28 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 1.6960 mL 8.4802 mL 16.9604 mL
5 mM 0.3392 mL 1.6960 mL 3.3921 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

纯度: 99.92%

COA (287 KB) HNMR (273 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Two days after transfection with siRNAs, medulloblastoma cells are seeded in a 96-well plate, and the following day, they are exposed to different doses of radiation. Cell viability is determined 72 hours after radiation treatment by MTT absorbance at 595 nm. For cells that are treated with M443 (250 nM, 500 nM), 6 hours after treatment with different concentrations of the drug or vehicle control, they are exposed to radiation and processed for the MTT assay 72 hours later as above. Five hundred cells are seeded in 6 cm dishes 2 days after siRNA transfections. The following day, cells are exposed to the different doses of radiation using a biologic irradiator and cultured for 7 days with media changes every other day. Colonies containing more than 50 cells are counted, and the results are used to calculate the surviving fractions. For the treatment with M443 or vehicle control, 24 hours after seeding, cells are exposed to the drug for 6 hours and subsequently to radiation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
The primary UI226 medulloblastoma cells are patient derived xenografts. UI226 is largely propagated as flank cultures in nude mice and cultured in StemPro media for less than 3 weeks before intracranial injections. Medulloblastoma cells (5.0×105 UI226 in 5 mL of StemPro medium) are injected over 5 minutes into the cerebellum of 4-week-old athymic female mice. Three weeks after tumor cell implantation and approximately 2 weeks before the animals become moribund; treatment is started by implantation of an osmotic pump filled with either 0.05 mg/mL solution of M443 or vehicle (0.01% DMSO in PBS) and implanted in a subcutaneous pocket on the dorsal flank of the animal. A catheter with attached cannula delivers the drug intracranially and directly into the tumor over a period of 2 weeks, at a steady rate of 0.25 mL/hour. Irradiation of the mice head is initiated 2 days after pump implantation and conducted over 2 days[1].

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

M443 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6960 mL 8.4802 mL 16.9604 mL 42.4009 mL
5 mM 0.3392 mL 1.6960 mL 3.3921 mL 8.4802 mL
10 mM 0.1696 mL 0.8480 mL 1.6960 mL 4.2401 mL
15 mM 0.1131 mL 0.5653 mL 1.1307 mL 2.8267 mL
20 mM 0.0848 mL 0.4240 mL 0.8480 mL 2.1200 mL
25 mM 0.0678 mL 0.3392 mL 0.6784 mL 1.6960 mL
30 mM 0.0565 mL 0.2827 mL 0.5653 mL 1.4134 mL
40 mM 0.0424 mL 0.2120 mL 0.4240 mL 1.0600 mL
50 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8480 mL
60 mM 0.0283 mL 0.1413 mL 0.2827 mL 0.7067 mL
80 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5300 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:

M4431820684-31-8M 443M-443Mixed Lineage KinaseMLKsInhibitorinhibitorinhibit

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