MRTX-1719
- CAS No.
- 2630904-45-7
- Chemical Name:
- MRTX-1719
- Synonyms
- Navlimetostat;BMS 986504;MRTX1719 ，E1024;navlimetostatum;MRTX-1719, 10 mM in DMSO;MRTX-1719,CRC,Histone Methyltransferase,NSCLC,Inhibitor,MTA,MRTX1719,MRTX 1719,inhibit,PRMT5;2-[4-[4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-5-pyrazolyl]-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;(2R)-2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;Benzonitrile, 2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1H-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2R)-
- CBNumber:
- CB29782000
- Molecular Formula:
- C23H18ClFN6O2
- Molecular Weight:
- 464.89
- MDL Number:
- MOL File:
- 2630904-45-7.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| MRTX-1719 ≥95% | 36563 | 1mg | $191 |
| MRTX-1719 ≥95% | 36563 | 5mg | $905 |
| MRTX-1719 ≥95% | 36563 | 10mg | $1142 |
| Navlimetostat 99.16% | CS-0226219 | 1mg | $227 |
| Navlimetostat 99.16% | CS-0226219 | 5mg | $932 |
| Density | 1.58±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility |
Acetonitrile: Soluble DMSO: Soluble |
| pka | 11.37±0.40(Predicted) |
| form | Solid |
| color | White to light yellow |
| InChIKey | BZKIOORWZAXIBA-UHFFFAOYSA-N |
| SMILES | CN1N=CC(C2=CC=C3C(NN=C(CN)C3=C2)=O)=C1C1C(=C(Cl)C=C(OC2CC2)C=1C#N)F |
MRTX-1719 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 36563 | MRTX-1719 ≥95% | 2630904-45-7 | 1mg | $191 | 2026-04-30 | Buy |
| Cayman Chemical | 36563 | MRTX-1719 ≥95% | 2630904-45-7 | 5mg | $905 | 2026-04-30 | Buy |
| Cayman Chemical | 36563 | MRTX-1719 ≥95% | 2630904-45-7 | 10mg | $1142 | 2026-04-30 | Buy |
| ChemScene | CS-0226219 | Navlimetostat 99.16% | 2630904-45-7 | 1mg | $227 | 2026-06-04 | Buy |
| ChemScene | CS-0226219 | Navlimetostat 99.16% | 2630904-45-7 | 5mg | $932 | 2026-06-04 | Buy |
MRTX-1719 Chemical Properties,Uses,Production
Uses
Navlimetostat is a potent, orally active, selective PRMT5MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5MTA and PRMT5. Navlimetostat binds to the PRMT5MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study[1][2].
Biological Activity
MRTX-1719 is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells[1].
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) | 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 |
| 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. |
IC 50
PRMT5
References
[1] Targeting the genetic and immunological drivers of cancer.
[2] CHRISTOPHER R. SMITH*. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers[J]. Journal of Medicinal Chemistry, 2022, 65 3: 1749-1766. DOI: 10.1021/acs.jmedchem.1c01900
MRTX-1719 Preparation Products And Raw materials
Raw materials
Preparation Products
MRTX-1719 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 20122 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32466 | 58 |
| BOC Sciences | 16314854226; +16314854226 | inquiry@bocsci.com | United States | 19853 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39040 | 58 |
| Chemtour Biotech Co., Ltd | +8617327281506 | market@chemtour.com | China | 1521 | 58 |
| SHANGHAI KEAN TECHNOLOGY CO., LTD. | +8613817748580 | cooperation@kean-chem.com | China | 40066 | 58 |
| Chengdu DingDang Pharmaceutical Co., Ltd. | 028-86040038 13980902949; | market@dingdangchem.com | China | 1854 | 55 |
| Suzhou Meidi Senuo Pharmaceutical Technology Co., Ltd. | 13771642864 | snhuyu_2008@126.com | China | 1189 | 58 |
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- MRTX-1719: Bioactivity and Chemical and studies
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