Art. -Nr.: HY-139611

Navlimetostat

(Synonyms: MRTX-1719; BMS-986504)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC₅₀ of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.

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Reinheit: 99.16%
CAS. Nr.: 2630904-45-7
Formel: C₂₃H₁₈ClFN₆O₂
Molecular Weight:464.88

Speicherung:

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

Navlimetostat Chemical Structure

CAS. Nr.: 2630904-45-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PRMT5

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	12 nM Compound: MRTX1719	Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as cell viability after 10 days by CellTiter-Glo assay Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as cell viability after 10 days by CellTiter-Glo assay	[PMID: 35926325]
HCT-116	IC₅₀	890 nM Compound: MRTX1719	Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as cell viability after 10 days by CellTiter-Glo assay Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as cell viability after 10 days by CellTiter-Glo assay	[PMID: 35926325]
HepG2	IC₅₀	6600 nM Compound: MRTX1719	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability measured after 120 hrs CellTiter-Glo assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability measured after 120 hrs CellTiter-Glo assay	[PMID: 35926325]

In Vitro

Navlimetostat (10 day) inhibits the PRMT5 activity and in MTAP-deleted HCT116 cells not wild type cells, with the IC₅₀ of 8 nM^[1]. Navlimetostat (10 day) inhibits the cell viability of MTAP del HCT116 cells with an IC₅₀ value of 12 nM and parental HCT116 cells with an IC₅₀ value of 890 nM^[1].

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

In Vivo

Navlimetostat (12.5-100 mg/kg/d for p.o., 21 day) reduces the tumor growth in Lu-99 orthotopic xenograft tumor models^[2].

Pharmacokinetic Analysis ^[2]

Model	Route	Dose (mg/kg)	Cl_total (mL/min/kg)	V_dss (L/kg)	t_1/2 (h)
CD-1 mouse.	i.v.	3	83	6.3	1.5
Beagle dog	i.v.	2	14	3.4	4.8
Cynomolgus monkey	i.v.	2	15	2.3	6.1

Model	Route	Dose (mg/kg)	C_max (ug/mL)	AUC_inf (h*ug/mL)	F (%)
CD-1 mouse.	p.o.	30	1.16	4.85	80
Beagle dog	p.o.	10	1.40	7.47	59
Cynomolgus monkey	p.o.	10	/	/	41

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

Animal Model:

Lu-99 (an MTAP/CDKN2A-deleted human lung cancer cell line ) xenograft tumor models^[2]

Dosage:

12.5, 25, 50, and 100 mg/kg/d, 21 day

Administration:

Oral gavage

Result:

Reduced the tumor volume with 86% tumor growth inhibition (TGI) at 50 mg/kg and 88% TGI at 100 mg/kg.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2630904-45-7
Appearance Solid
Molecular Weight 464.88
Formel C₂₃H₁₈ClFN₆O₂
Color White to light yellow
SMILES

FC1=C(C=C(C(C#N)=[C@]1[C@]2=C(C3=CC=C4C(C(CN)=NNC4=O)=C3)C=NN2C)OC5CC5)Cl
Synonyms

MRTX-1719; BMS-986504
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (3)

All Cell Migration/Invasion AssayCell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

MedComm (2020)

SCR-7952, a highly selective MAT2A inhibitor, demonstrates synergistic antitumor activities in combination with the S-adenosylmethionine-competitive or the methylthioadenosine-cooperative protein arginine methyltransferase 5 inhibitors in methylthioadenosine phosphorylase-deleted tumors. [Abstract]

2024 Sep 20;5(10):e705. PMID: 39309689

Navlimetostat purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Sep 20;5(10):e705. [Abstract]

Drug dose-response curves for proliferation inhibition and Bliss plots showing the synergistic effects of SCR-7952 in combination with MRTX-1719 on HCT116 MTAP^-/-cells over 8 days.
Cancer Med

Inhibitory Effect of PRMT5/MTA Inhibitor on MTAP-Deficient Glioma May Be Influenced by Surrounding Normal Cells. [Abstract]

2024 Dec;13(24):e70526. PMID: 39711357

Navlimetostat purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526. [Abstract]

MRTX1719 (0–10000 nM, 8 days) inhibited the growth of the above five cell types.

Navlimetostat purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526. [Abstract]

MRTX1719 (0–10000 nM, 14 days) inhibited the growth of the above four cell types.

Navlimetostat purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526. [Abstract]

Following subcutaneous injection of MRTX1719 (10 mg/kg, intraperitoneal injection), the drug concentration in the brain reached its maximum approximately 1 h after administration. The brain-to-plasma concentration ratio of MRTX1719 peaked at 4 h post-administration (brain (A) and serum (B); brain-to-plasma concentration ratio (C)).

Navlimetostat purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526. [Abstract]

MRTX1719 (10 mg/kg, intraperitoneal injection) reduced the volume of Hs683-transplanted tumors without reducing the body weight of the mice.
Research Square Preprint

2024 Nov 06.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (215.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1511 mL

10.7555 mL

21.5109 mL

5 mM

0.4302 mL

2.1511 mL

4.3022 mL

10 mM

0.2151 mL

1.0755 mL

2.1511 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2 mg/mL (4.30 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lars D Engstrom, et al. MRTX1719 is an MTA-cooperative PRMT5 inhibitor that exhibits synthetic lethality in preclinical models and patients with MTAP deleted cancer. Cancer Discov. 2023 Aug 8;CD-23-0669. [Content Brief]

[2]. Christopher R Smith, et al. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers. J Med Chem. 2022 Feb 10;65(3):1749-1766. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1511 mL	10.7555 mL	21.5109 mL	53.7773 mL
	5 mM	0.4302 mL	2.1511 mL	4.3022 mL	10.7555 mL
	10 mM	0.2151 mL	1.0755 mL	2.1511 mL	5.3777 mL
	15 mM	0.1434 mL	0.7170 mL	1.4341 mL	3.5852 mL
	20 mM	0.1076 mL	0.5378 mL	1.0755 mL	2.6889 mL
	25 mM	0.0860 mL	0.4302 mL	0.8604 mL	2.1511 mL
	30 mM	0.0717 mL	0.3585 mL	0.7170 mL	1.7926 mL
	40 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3444 mL
	50 mM	0.0430 mL	0.2151 mL	0.4302 mL	1.0755 mL
	60 mM	0.0359 mL	0.1793 mL	0.3585 mL	0.8963 mL
	80 mM	0.0269 mL	0.1344 mL	0.2689 mL	0.6722 mL
	100 mM	0.0215 mL	0.1076 mL	0.2151 mL	0.5378 mL

Keywords

Navlimetostat

3 Cited Publications

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Navlimetostat

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Navlimetostat

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Navlimetostat

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Navlimetostat

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Navlimetostat Related Classifications

HY-139611 Related Classifications