MT-DADMe-ImmA (Synonyms: MTDIA; Methylthio-DADMe-Immucillin A)

Name: MT-DADMe-ImmA
Brand: MedChemExpress
SKU: HY-101496
Rating: 5.0 (3 reviews)

Cat. No.: HY-101496 Purity: 98.42%: Data Sheet
SDS

COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a K_i of 90 pM.

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

MT-DADMe-ImmA Chemical Structure

CAS No. : 653592-04-2

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

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE MT-DADMe-ImmA

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•Related Screening Libraries:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a K_i of 90 pM.

IC₅₀ & Target

Ki: 90 pM (MTAP)^[1]

In Vitro

Treatment of cultured cells with MT-DADMe-ImmA and MTA inhibit MTAP, increase cellular MTA concentrations, decrease polyamines, and induce apoptosis in FaDu and Cal27, two head and neck squamous cell carcinoma cell lines. The same treatment does not induce apoptosis in normal human fibroblast cell lines (CRL2522 and GM02037) or in MCF7, a breast cancer cell line with an MTAP gene deletion. MT-DADMe-ImmA alone does not induce apoptosis in any cell line, implicating MTA as the active agent^[2].

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

In Vivo

The t_1/2 for onset of inhibition is 50 min with complete inhibition by 250 min. MTAP activity slowly returns, giving a biological half-life for the action of oral MT-DADMe-ImmA of 6.3 days. The time-dependent growth of FaDu tumors in immunodeficient mice is suppressed by oral or intraperitoneal treatment with MT-DADMe-ImmA^[2].

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

Molecular Weight

293.40

Formula

C₁₃H₁₉N₅OS

CAS No.

653592-04-2

Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1CN(CC2=CNC3=C(N)N=CN=C32)C[C@@H]1CSC

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 (340.84 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	3.4084 mL	17.0418 mL	34.0836 mL
5 mM	0.6817 mL	3.4084 mL	6.8167 mL
10 mM	0.3408 mL	1.7042 mL	3.4084 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.52 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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 98.42%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (251 KB) HNMR (259 KB) RP-HPLC (207 KB) MS (68 KB) OR (231 KB)

Handling Instructions (2659 KB)

References

[1]. Evans GB, et al. Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase. J Med Chem. 2005 Jul 14;48(14):4679-89. [Content Brief]

[2]. Basu I, et al. A transition state analogue of 5'-methylthioadenosine phosphorylase induces apoptosis in head and neck cancers. J Biol Chem. 2007 Jul 20;282(29):21477-86. [Content Brief]

Cell Assay ^[2]	Cell viability is evaluated using the Alamar Blue assay. Cells are seeded onto 96-well plates at a density of 104 cells/well and incubated with increasing concentrations of MT-DADMe-ImmA (100 pM to 100 μM) for 4 days at fixed MTA concentrations (0, 5, 10, and 20 μM). IC₅₀ is determined with the assay data^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Tumors were established in mice for 5 days prior to oral or intraperitoneal treatments with MT-DADMe-ImmA. Mice are treated with oral dose of 21 mg/kg or an intraperitoneal dose of 5 mg/kg/day MT-DADMe-ImmA^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Evans GB, et al. Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase. J Med Chem. 2005 Jul 14;48(14):4679-89. [Content Brief] [2]. Basu I, et al. A transition state analogue of 5'-methylthioadenosine phosphorylase induces apoptosis in head and neck cancers. J Biol Chem. 2007 Jul 20;282(29):21477-86. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4084 mL	17.0418 mL	34.0836 mL	85.2091 mL
	5 mM	0.6817 mL	3.4084 mL	6.8167 mL	17.0418 mL
	10 mM	0.3408 mL	1.7042 mL	3.4084 mL	8.5209 mL
	15 mM	0.2272 mL	1.1361 mL	2.2722 mL	5.6806 mL
	20 mM	0.1704 mL	0.8521 mL	1.7042 mL	4.2605 mL
	25 mM	0.1363 mL	0.6817 mL	1.3633 mL	3.4084 mL
	30 mM	0.1136 mL	0.5681 mL	1.1361 mL	2.8403 mL
	40 mM	0.0852 mL	0.4260 mL	0.8521 mL	2.1302 mL
	50 mM	0.0682 mL	0.3408 mL	0.6817 mL	1.7042 mL
	60 mM	0.0568 mL	0.2840 mL	0.5681 mL	1.4202 mL
	80 mM	0.0426 mL	0.2130 mL	0.4260 mL	1.0651 mL
	100 mM	0.0341 mL	0.1704 mL	0.3408 mL	0.8521 mL

MT-DADMe-ImmA Related Classifications

Keywords:

MT-DADMe-ImmA653592-04-2MTDIA Methylthio-DADMe-Immucillin AHistone MethyltransferaseInhibitorinhibitorinhibit

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MT-DADMe-ImmA (Synonyms: MTDIA; Methylthio-DADMe-Immucillin A)

Customer Review

3 Publications Citing Use of MCE MT-DADMe-ImmA

Featured Recommendations

•Related Screening Libraries:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

MT-DADMe-ImmA Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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SAFETY DATA SHEET (SDS)

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