1. Stem Cell/Wnt
  2. Smo
  3. MRT-10

MRT-10 是一种七跨膜平滑受体 (Smo) 拮抗剂,在各种 Hedgehog (Hh) 测定中,IC50 为 0.65 μM。MRT-10 在 Bodipycyclopamine 结合位点水平与 Smo 受体结合。MRT-10可用于癌症研究。

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MRT-10 Chemical Structure

MRT-10 Chemical Structure

CAS No. : 330829-30-6

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
C3H 10T1/2 IC50
0.868 μM
Compound: 2; MRT-10
Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs
Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs
10.1039/C5MD00092K
C3H 10T1/2 IC50
0.9 μM
Compound: 1a
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
[PMID: 22268551]
HEK293 IC50
0.281 μM
Compound: 2; MRT-10
Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
10.1039/C5MD00092K
HEK293 IC50
300 nM
Compound: 1a
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
[PMID: 22268551]
HT-29 IC50
6.61 μM
Compound: 2; MRT-10
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay
10.1039/C5MD00092K
MGC-803 IC50
8.62 μM
Compound: 2; MRT-10
Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay
10.1039/C5MD00092K
Shh Light II IC50
0.65 μM
Compound: 1a
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
[PMID: 22268551]
SW-620 IC50
21.23 μM
Compound: 2; MRT-10
Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay
10.1039/C5MD00092K
体外研究
(In Vitro)

MRT-10 inhibits the Smo-induced IP accumulation in a dosedependent manner (IC50=2.5 μM) in HEK293 cells[1].
MRT-10 (10-9-10-5 M; 2 h) blocks Bodipy-cyclopamine (5 nM; 2 h) binding to cells expressing mouse Smo in a dosedependent manner with an IC50=0.5 μM[1].
MRT-10 (10-9-10-5 M; 40 h) inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with an IC50=0.64 μM[1].
MRT-10 (10-9-10-5 M; 6 days) inhibits the SAG-induced (0.1 μM) alkaline phosphatase (AP) activity with an IC50=0.90 μM ) in C3H10T1/2 cells[1].

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

分子量

465.52

Formula

C24H23N3O5S

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
4°C 2 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 : 100 mg/mL (214.81 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 2.1481 mL 10.7407 mL 21.4814 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 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

动物实验:

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: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.37 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    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。

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

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
参考文献

MRT-10 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 2.1481 mL 10.7407 mL 21.4814 mL 53.7034 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 mL 10.7407 mL
10 mM 0.2148 mL 1.0741 mL 2.1481 mL 5.3703 mL
15 mM 0.1432 mL 0.7160 mL 1.4321 mL 3.5802 mL
20 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1481 mL
30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7901 mL
40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 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.

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