MRTX-1719 manufacturers
- MRTX-1719
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- $8.00
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2026-09-02
- CAS:2630904-45-7
- Min. Order: 1kg
- Purity: 99%
- MRTX-1719
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- $172.00
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2026-07-14
- CAS:2630904-45-7
- Purity: 99.03%
- Supply Ability: 10g
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| | MRTX-1719 Basic information |
| Product Name: | MRTX-1719 | | Synonyms: | 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)-;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;(2R)-2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;MRTX-1719, 10 mM in DMSO;BMS 986504;navlimetostatum;MRTX1719 ，E1024 | | CAS: | 2630904-45-7 | | MF: | C23H18ClFN6O2 | | MW: | 464.89 | | EINECS: | | | Product Categories: | | | Mol File: | 2630904-45-7.mol |  |
| | MRTX-1719 Chemical Properties |
| 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 Usage And Synthesis |
| 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 |
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