Navlimetostat (Synonyms: MRTX-1719; BMS-986504)

Name: Navlimetostat
Brand: MedChemExpress
SKU: HY-139611
Rating: 5.0 (3 reviews)

Cat. No.: HY-139611 Purity: 99.16%: Data Sheet
COA

SDS
Handling Instructions
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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.

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

CAS No. : 2630904-45-7

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

Other Forms of Navlimetostat:

(S)-Navlimetostat In-stock
Navlimetostat hydrochloride In-stock

3 Publications Citing Use of MCE Navlimetostat

Cell Migration/Invasion Assay

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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.

: 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.

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•Related Screening Libraries:

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PRMT5

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	12 nM Compound: (M)-27; MRTX1719	Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
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	3470 nM Compound: (P)-27	Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
HCT-116	IC₅₀	41 nM Compound: 27	Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
HCT-116	IC₅₀	890 nM Compound: (M)-27; MRTX1719	Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
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]
HCT-116	IC₅₀	> 10000 nM Compound: (P)-27	Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
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

Molecular Weight

464.88

Formula

C₂₃H₁₈ClFN₆O₂

CAS No.

2630904-45-7

Appearance

Solid

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

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 (215.11 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	2.1511 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

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 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.
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 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.
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 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

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: 99.28%

Select Batch:

Data Sheet (286 KB) SDS (254 KB)

COA (260 KB) HNMR (273 KB) RP-HPLC (197 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Navlimetostat 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:

Navlimetostat2630904-45-7MRTX-1719 BMS-986504MRTX1719MRTX 1719BMS986504BMS 986504BMS-986504Histone MethyltransferaseNSCLCCRCPRMT5MTAHCT116Lu-99Inhibitorinhibitorinhibit

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Navlimetostat (Synonyms: MRTX-1719; BMS-986504)

Customer Review

Other Forms of Navlimetostat:

Navlimetostat Related Antibodies

3 Publications Citing Use of MCE Navlimetostat

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Navlimetostat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Navlimetostat Related Classifications

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