≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor
In Vitro
MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC 50 3 nM; prolif. IC 50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC 50 544 nM; prolif. IC 50 861 nM). MRTX9768 (0-250 nM) results in LU99 SDMA inhibition maintaining after 3-hr drug treatment followed by 4-day washout (exhibiting tight binding and prolonged PRMT5•MTA occupancy). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow . MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors (such as glioblastoma). MRTX9768 (PO dose 30 mg/kg in CD-1 mouse and beagle dog, 10 mg/kg in cynomolgus monkey) has a favorable ADME profile (>50% bioavailability in mice and dogs, moderate to high clearance, No changes in RBC parameters when administered well above efficacious concentrations (1000 mg/kg)). MRTX9768 (100 mg/kg, orally, BID, 6/21 days) results in SDMA inhibition maintaining 3 days after dosing is stopped. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:PRMT5•MTA
| Canonical Smiles | CN1C(=C(C=N1)C2=CC3=C(C=C2)C(=O)NN=C3CN)C4=C(C5=CC=CC=C5C=C4F)C#N |
|---|---|
| IUPAC Name | 2-[4-[4-(aminomethyl)-1-oxo-2H-phthalazin-6-yl]-2-methylpyrazol-3-yl]-3-fluoronaphthalene-1-carbonitrile |
| InChIKey | BPTYWAYMKBEXES-UHFFFAOYSA-N |
| INCHI | 1S/C24H17FN6O/c1-31-23(22-18(10-26)15-5-3-2-4-13(15)9-20(22)25)19(12-28-31)14-6-7-16-17(8-14)21(11-27)29-30-24(16)32/h2-9,12H,11,27H2,1H3,(H,30,32) |
| Isomeric SMILES | CN1C(=C(C=N1)C2=CC3=C(C=C2)C(=O)NN=C3CN)C4=C(C5=CC=CC=C5C=C4F)C#N |
| PubChem CID | 156151804 |
| Molecular Weight | 424.43 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Solubility | DMSO : 50 mg/mL (117.81 mM; ultrasonic and warming and heat to 60°C) |
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