Navlimetostat hydrochloride
Based on 5 publication(s) in Google Scholar
Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride 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.
- Purity : 99.89%
- Formula: C23H19Cl2FN6O2
- Molecular Weight:501.34
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Navlimetostat hydrochloride
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
All Histone Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
PRMT5 |
In Vitro
Navlimetostat (10 day) hydrochloride inhibits the PRMT5 activity and in MTAP-deleted HCT116 cells not wild type cells, with the IC50 of 8 nM[1].
Navlimetostat (10 day) hydrochloride 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
Pharmacokinetic Analysis [2]
| Model | Route | Dose (mg/kg) | Cltotal (mL/min/kg) | Vdss (L/kg) | t1/2 (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) | Cmax (ug/mL) | AUCinf (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.
Chemical Information
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Appearance Solid
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Molecular Weight 501.34
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Formula C23H19Cl2FN6O2
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Color White to off-white
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SMILES
[H]Cl.FC1=C(C=C(C(C#N)=[C@]1[C@]2=C(C3=CC=C4C(C(CN)=NNC4=O)=C3)C=NN2C)OC5CC5)Cl
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Synonyms
MRTX-1719 hydrochloride; BMS-986504 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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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 hydrochloride 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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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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.
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Histol Histopathol
Targeting of CDK1 and PRMT5 as a potential therapeutic combination for non-small cell lung cancer. [Abstract]2026 Jul;41(7):1275-1288. PMID: 41487038 -
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (99.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.49 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.49 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (288 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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
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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.9947 mL | 9.9733 mL | 19.9465 mL | 49.8664 mL |
| 5 mM | 0.3989 mL | 1.9947 mL | 3.9893 mL | 9.9733 mL | |
| 10 mM | 0.1995 mL | 0.9973 mL | 1.9947 mL | 4.9866 mL | |
| 15 mM | 0.1330 mL | 0.6649 mL | 1.3298 mL | 3.3244 mL | |
| 20 mM | 0.0997 mL | 0.4987 mL | 0.9973 mL | 2.4933 mL | |
| 25 mM | 0.0798 mL | 0.3989 mL | 0.7979 mL | 1.9947 mL | |
| 30 mM | 0.0665 mL | 0.3324 mL | 0.6649 mL | 1.6622 mL | |
| 40 mM | 0.0499 mL | 0.2493 mL | 0.4987 mL | 1.2467 mL | |
| 50 mM | 0.0399 mL | 0.1995 mL | 0.3989 mL | 0.9973 mL | |
| 60 mM | 0.0332 mL | 0.1662 mL | 0.3324 mL | 0.8311 mL | |
| 80 mM | 0.0249 mL | 0.1247 mL | 0.2493 mL | 0.6233 mL |
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