2. MAPK/ERK Pathway Autophagy
  3. Mixed Lineage Kinase Autophagy
  4. URMC-099

URMC-099 是一种口服生物有效的混合谱系激酶 3 (MLK3) (IC50=14 nM) 抑制剂，具有优异的血脑屏障穿透性。

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URMC-099 Chemical Structure

URMC-099 Chemical Structure

CAS No. : 1229582-33-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1089
In-stock
1 mg ￥450
In-stock
5 mg ￥990
In-stock
10 mg ￥1500
In-stock
50 mg ￥4000
In-stock
100 mg ￥6950
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

URMC-099 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

URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.

IC50 & Target

LRRK2

11 nM (IC50)

FLT3

4 nM (IC50)

FLT1

39 nM (IC50)

ABL1 (T315I)

3 nM (IC50)

ABL1

6.8 nM (IC50)

SGK

67 nM (IC50)

SGK1

201 nM (IC50)

AurA

108 nM (IC50)

AurB

123 nM (IC50)

AurC

290 nM (IC50)

IKKβ

257 nM (IC50)

IKKα

591 nM (IC50)

TNFα

460 nM (IC50)

ROCK1

1030 nM (IC50)

ROCK2

111 nM (IC50)

CDK1

1125 nM (IC50)

CDK2

1180 nM (IC50)

TRKA

85 nM (IC50)

c-MET

177 nM (IC50)

TRKB

217 nM (IC50)

IGF1R

307 nM (IC50)

LCK

333 nM (IC50)

MEKK2

661 nM (IC50)

SYK

731 nM (IC50)

AMPK

1512 nM (IC50)

JNK1

3280 nM (IC50)

SRC

4330 nM (IC50)

ZAP70

5050 nM (IC50)

ERK2

6290 nM (IC50)

P38α

12050 nM (IC50)

CYP3A4

16.2 μM (IC50)

体外研究
(In Vitro)

The effect of URMC-099 (URMC099) on the in vitro growth of the “brain homing” MDA-MB-231 BR cells expressing eGFP (eGFP8.4) and their parental cell line, MDA-MB-231 is tested. The cells are treated with either 200 nM URMC-099 or vehicle alone. Cells treated with URMC-099 grow at a similar rate to those treated with vehicle. Cell viability is >99% in all cases[2].

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

URMC-099 相关抗体:
体内研究
(In Vivo)

URMC-099 has moderate terminal elimination half-life (t1/2=1.92 h, 2.14 h and 2.72 h for C57 BL/6 mice (10 mg/kg, oral dosing), C57 BL/6 mice (2.5 mg/kg, iv), C57 BL/6 mice (10 mg/kg, iv))[1]. The effect of URMC-099 (URMC099) on tumor formation in vivo is analyzed using a well characterized mouse xenograft model of breast cancer brain metastasis. For these experiments, eGFP8.4 cells are inoculated into the left ventricle of immunodeficient nu/nu mice; animals are then treated with either URMC-099 (10 mg/kg) or vehicle alone, every 12 hours for 20 days. This dose of URMC-099 is chosen because it has been shown to be sufficient to effectively inhibit MLK3 in mice, with good penetration of the blood-brain barrier and potent inhibition of the phosphorylation of Jun N-terminal kinase (JNK) in brain tissue. On day 21 the mice are sacrificed and number of BM is assessed. Fifteen mice are used for each treatment group. BM are detected in 60% of mice, which is consistent with previous studies using this xenograft model by other investigators. URMC-099 treatment significantly (p<0.05, two-tailed t-test) increases the total number of brain metastasis (BM) in mice. For micrometastases, the pattern is similar to that observed for total BM. The number of macrometastases is statistically indistinguishable between mice treated with URMC-099 or vehicle[2].

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

421.54

Formula

C27H27N5
CAS 号
性状

固体

颜色

Off-white 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
In Vitro: 

DMSO 中的溶解度 : ≥ 33 mg/mL (78.28 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3723 mL 11.8613 mL 23.7225 mL
5 mM 0.4745 mL 2.3723 mL 4.7445 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

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

  • 方案 一

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.87 mg/mL (6.81 mM); 澄清溶液

  • 方案 二

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.87 mg/mL (6.81 mM); 澄清溶液

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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.34%

COA (198 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

MDA-MB-231, MCF10A, HS578t and MDA-MB-231 EGFP8.4 cells are seeded in a 24 well plate at an initial density of 5.0×104 cells/mL in 0.5 mL of media. The cells are treated with either 200 µM of URMC-099 or vehicle (0.002% DMSO). Cell number in each well is measured by trypsinizing the cells and counting them with a hematocytometer. The viability is tested by trypan blue dye exclusion. Each condition is tested in triplicate[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
6 to 8 week old female nu/nu mice are injected intraperitoneally with URMC-099 at a dose of 10 mg/kg, or vehicle, twice daily for 20 days. On day 21 mice are sacrificed by CO2 suffocation. Brains are removed and fixed with 4% formaldehyde in PBS overnight, then transferred to 30% sucrose in PBS. The brains are then quickly frozen by immersing into isopentane cooled on dry ice. The frozen brains are sectioned coronally every 30 micrometers. Eight sections starting at bregma 2.0 and separated by 360 µm are mounted on glass slides for tumor evaluation under the microscope. The number of brain metastasis (BM) is counted by examining eGFP signals under a fluorescence microscope at 20× magnification[2].

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

URMC-099 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 2.3723 mL 11.8613 mL 23.7225 mL 59.3064 mL
5 mM 0.4745 mL 2.3723 mL 4.7445 mL 11.8613 mL
10 mM 0.2372 mL 1.1861 mL 2.3723 mL 5.9306 mL
15 mM 0.1582 mL 0.7908 mL 1.5815 mL 3.9538 mL
20 mM 0.1186 mL 0.5931 mL 1.1861 mL 2.9653 mL
25 mM 0.0949 mL 0.4745 mL 0.9489 mL 2.3723 mL
30 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9769 mL
40 mM 0.0593 mL 0.2965 mL 0.5931 mL 1.4827 mL
50 mM 0.0474 mL 0.2372 mL 0.4745 mL 1.1861 mL
60 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9884 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:

URMC-0991229582-33-5URMC099URMC 099Mixed Lineage KinaseAutophagyMLKsInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-12599
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