Navlimetostat (also known as MRTX1719 or BMS-986504) is a potent and selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), specifically designed to target PRMT5 activity in tumors harboring methylthioadenosine phosphorylase (MTAP) deletion. Navlimetostat demonstrates nanomolar inhibitory potency against PRMT5 (IC₅₀ ≈ 2–6 nM) and shows preferential anti-proliferative effects in MTAP-null cancer cell lines, exploiting synthetic lethality by leveraging elevated levels of methylthioadenosine (MTA), which partially inhibits PRMT5. In MTAP-deleted xenograft models, Navlimetostat significantly reduces tumor growth with tolerable systemic exposure and minimal toxicity.
MedKoo Cat#: 465753
Name: Navlimetostat
CAS#: 2630904-45-7
Chemical Formula: C23H18ClFN6O2
Exact Mass: 464.1164
Molecular Weight: 464.89
Elemental Analysis: C, 59.42; H, 3.90; Cl, 7.63; F, 4.09; N, 18.08; O, 6.88
The following data is based on the product molecular weight 464.89 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
