MRT-10

Name: MRT-10
Brand: MedChemExpress
SKU: HY-108507
Rating: 4.5 (1 reviews)

Cat. No.: HY-108507 Purity: 98.99%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

MRT-10 Chemical Structure

CAS No. : 330829-30-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 184	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 184	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

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

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].

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

Molecular Weight

465.52

Formula

C₂₄H₂₃N₃O₅S

CAS No.

330829-30-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC(NC1=CC=CC(NC(C2=CC=CC=C2)=O)=C1)=S)C3=CC(OC)=C(OC)C(OC)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (214.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2148 mL	1.0741 mL	2.1481 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.99%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (246 KB) HNMR (250 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Manetti F, et al. Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists. Mol Pharmacol. 2010 Oct;78(4):658-65. [Content Brief]

[2]. Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012 Feb 23;55(4):1559-71. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

MRT-10 Related Classifications

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:

MRT-10330829-30-6MRT10MRT 10SmoSmoothenedcancerSmo-induced IP accumulationBodipy-cyclopamineShhN signalingSAG-induced AP activityInhibitorinhibitorinhibit

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MRT-10

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Complete Stock Solution Preparation Table

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