| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
PRMT5
MRTX‑1719 hydrochloride targets the PRMT5/MTA complex, a protein complex involved in protein arginine methylation. The compound binds to the PRMT5‑MTA complex with exceptionally high affinity (Kd = 0.14 pM). By inhibiting this complex, it selectively inhibits PRMT5‑dependent SDMA modification in MTAP‑deleted cancer cells. This selective targeting exploits the synthetic lethality between MTAP deletion and PRMT5 inhibition. |
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| ln Vitro |
In vitro, MRTX‑1719 hydrochloride shows selective, dose‑dependent inhibition of PRMT5‑dependent SDMA modification in MTAP‑deleted cancer cell lines. It exhibits potent antiproliferative activity against MTAP‑deleted cancer cells, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells. The compound shows antineoplastic activity in a panel of MTAP‑deleted cell line models.
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| ln Vivo |
In vivo, MRTX‑1719 hydrochloride (12.5, 25, 50, and 100 mg/kg, once daily for 22 days) exhibits selective, dose‑dependent inhibition of PRMT5‑dependent SDMA modification in MTAP‑deleted tumor xenografts. It is administered via daily oral gavage to immunocompromised mice bearing LU99 tumor xenografts. The compound shows antineoplastic activity in vivo.
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| Enzyme Assay |
Non‑cellular binding assays for MRTX‑1719 hydrochloride involve measuring its binding affinity to the PRMT5‑MTA complex using surface plasmon resonance (SPR). The compound is incubated with the PRMT5‑MTA complex, and the binding affinity (Kd = 0.14 pM) is determined from binding curves. Selectivity for PRMT5‑MTA over PRMT5‑SAM can also be assessed.
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| Cell Assay |
In vitro cellular assays for MRTX‑1719 hydrochloride are performed using MTAP‑deleted and MTAP wild‑type cancer cell lines. Cells are treated with the compound for 5 days, and cell viability is assessed to determine potency. PRMT5‑dependent SDMA modification is measured by Western blotting to confirm target engagement.
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| Animal Protocol |
In vivo animal experiments for MRTX‑1719 hydrochloride are conducted in immunocompromised mice bearing LU99 tumor xenografts. The compound is administered via daily oral gavage at doses of 12.5, 25, 50, and 100 mg/kg for 22 days. Endpoints include tumor growth inhibition and assessment of SDMA modification in tumor tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for MRTX‑1719 hydrochloride have been characterized in vivo. Despite low permeability and a high efflux ratio in MDCK assays, the compound was advanced to in vivo PK studies. The compound is administered via oral gavage. Detailed PK parameters such as half‑life and bioavailability are not extensively detailed in available sources.
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| Toxicity/Toxicokinetics |
Toxicological data for MRTX‑1719 hydrochloride are not extensively detailed in available sources. As a potent inhibitor of the PRMT5/MTA complex, it may have on‑target toxicities related to the inhibition of protein arginine methylation. The compound is intended for research use only and not for human consumption. Comprehensive toxicological studies would be required for any therapeutic development.
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| References | |
| Additional Infomation |
MRTX‑1719 hydrochloride (Navlimetostat hydrochloride) is a potent, first‑in‑class, selective inhibitor of the PRMT5/MTA complex with an IC50 of less than 10 nM in MTAP‑deleted cells. It binds to the PRMT5‑MTA complex with a Kd of 0.14 pM. It shows antineoplastic activity in vitro and in vivo and can be used for cancer research. It is not approved for clinical use.
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| Molecular Formula |
C23H19CL2FN6O2
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| Molecular Weight |
501.34
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| Related CAS # |
MRTX-1719;2630904-45-7
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| Appearance |
White to off-white solid powder
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| Synonyms |
Navlimetostat HCl; MRTX-1719 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~199.47 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9947 mL | 9.9733 mL | 19.9465 mL | |
| 5 mM | 0.3989 mL | 1.9947 mL | 3.9893 mL | |
| 10 mM | 0.1995 mL | 0.9973 mL | 1.9947 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT07544628
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT07579221
Conditions:Non-Small Cell Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT07382544
Conditions:Advanced Cancer|Solid Tumor
Title:Phase 1 Study of MRTX1719 in Solid Tumors With MTAP Deletion
Status:Recruiting
updateDate:2025-12-05
Ctid:NCT05245500
Link: https://clinicaltrials.gov/ct2/show/NCT05245500
Conditions:Mesothelioma|Non Small Cell Lung Cancer|Malignant Peripheral Nerve Sheath Tumors|Solid Tumor|Pancreatic Adenocarcinoma|Advanced Solid TumorProducts are for research use only; We do not sell to patients
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