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MRTX-1719

Name: MRTX-1719
Brand: TargetMol
SKU: T40254
Price: 172 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T40254Cas No. 2630904-45-7

MRTX-1719 is a potent and selective inhibitor of the PRMT5/MTA complex with an IC50 value of <10 nM against PRMT5/MTAMTAPDELSDMA cell lines.

MRTX-1719

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Purity: 99.18%

Catalog No. T40254Cas No. 2630904-45-7

MRTX-1719 is a potent and selective inhibitor of the PRMT5/MTA complex with an IC50 value of <10 nM against PRMT5/MTAMTAPDELSDMA cell lines.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$172	In Stock	In Stock
5 mg	$712	In Stock	In Stock
10 mg	$959	In Stock	In Stock
25 mg	$1,590	In Stock	In Stock
50 mg	$2,230	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$728	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.18%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR

Product Introduction

MRTX-1719 AI Summary

MRTX-1719 demonstrates significant pharmacological properties, including low apparent permeability and high efflux ratio in dog MDCKII-MDR1 cells. Notably, it effectively inhibits PRMT5 methyltransferase activity in human HCT-116 cells (MTAP knockout) with an IC50 value of approximately 8.0 nM and exhibits antiproliferative activity with IC50 values around 12.0 nM. In wild type HCT-116 cells, its antiproliferative and PRMT5 inhibition IC50 values are significantly higher, indicating selectivity for MTAP knockout cells. Additionally, the compound binds PRMT5 in the presence of MTA and SAM, shows moderate to high intrinsic clearance in hepatocytes, and demonstrates good oral bioavailability in animal models including CD-1 mice, beagle dogs, and cynomolgus monkeys. In preclinical models, MRTX-1719 shows antitumor activity against MTAP/CDKN2A-deleted human Lu-99 xenografts in athymic nude mice. Furthermore, it exhibits antiproliferative activity against human HepG2 cells with an IC50 of 6600.0 nM and maintains metabolic stability with a human hepatocyte clearance rate of less than 18.0 mL.min^-1.kg^-1..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	MRTX-1719 is a potent and selective inhibitor of the PRMT5/MTA complex with an IC50 value of <10 nM against PRMT5/MTAMTAPDELSDMA cell lines.
Targets&IC50	PRMT5/MTAMTAPDELSDMA cells:<10 nM (IC50)
In vitro	METHODS: To study the selectivity of MRTX1719 in reducing MTAP del tumor cell viability, 70 MTAP del and 26 MTAP WT human cancer cell lines were evaluated in a 5-day CellTiter-Glo (CTG) viability assay. RESULTS MRTX1719 selectively reduced the viability of MTAP del cell line, with minimal impact on MTAP WT cells. The median IC50 value of MRTX1719 in MTAP del cell line was 90 nmol/L, while the median IC50 value of MRTX1719 in MTAP WT cell line was IC50 is 2.2 μmol/L. [1] METHODS: MRTX1719 was studied in MTAP-del SDMA cells and MTAP-del active cell experiments. RESULTS IC50 = 8 nM in the MTAP-del SDMA experiment and IC50 = 12 nM in the MTAP-del activity experiment, with 82-fold and 74-fold selectivity over the corresponding MTAPWT experiment. [2]
In vivo	METHODS: MRTX1719 was studied in selected MTAP del cell line-derived xenograft (CDX) and patient-derived xenograft (PDX) models for ∼3 weeks at 100 mg/kg orally. RESULTS MRTX1719 showed significant anti-tumor activity in all models tested. [1] METHODS: Lu-99 is a human lung cancer cell line lacking MTAP/cdkn2a. When tumors reached ~200 mm3, MRTX1719 was administered by gavage (12.5, 25, 50, and 100 mg/kg) once daily until day 21. Tumor volumes were measured throughout the study. RESULTS MRTX1719 can inhibit the growth of Lu-99 cells in a concentration-dependent manner. [2]

Chemical Properties

Molecular Weight	464.88
Formula	C₂₃H₁₈ClFN₆O₂
Cas No.	2630904-45-7
Smiles	CN1C(=C(C=N1)C=2C=C3C(=CC2)C(=O)NN=C3CN)C4=C(C#N)C(OC5CC5)=CC(Cl)=C4F
Relative Density.	1.58 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 83.33 mg/mL (179.25 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.3 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1511 mL	10.7555 mL	21.5109 mL	107.5546 mL
5 mM	0.4302 mL	2.1511 mL	4.3022 mL	21.5109 mL
10 mM	0.2151 mL	1.0755 mL	2.1511 mL	10.7555 mL
20 mM	0.1076 mL	0.5378 mL	1.0755 mL	5.3777 mL
50 mM	0.0430 mL	0.2151 mL	0.4302 mL	2.1511 mL
100 mM	0.0215 mL	0.1076 mL	0.2151 mL	1.0755 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc