Vopimetostat, also known as TNG462, is a potent, selective PRMT5 inhibitor that exploits synthetic lethality in MTAP-deleted cancer cells by targeting the PRMT5–MTA (methylthioadenosine) complex. It demonstrates high biochemical potency, with an IC₅₀ of ~1.1 nM against PRMT5 in vitro, and exhibits enhanced selectivity for MTAP-null cells due to MTA accumulation. Cellular assays show TNG462 significantly reduces symmetric dimethylarginine (sDMA) levels and inhibits proliferation in MTAP-deleted tumor cell lines with GI₅₀ values typically in the low nanomolar range (e.g., 10–30 nM), while sparing MTAP-wildtype cells. In xenograft models of MTAP-deleted tumors, TNG462 induces marked tumor regression without significant toxicity, validating its therapeutic potential as a biomarker-driven epigenetic therapy.
MedKoo Cat#: 126755
Name: TNG462
CAS#: 2760483-96-1
Chemical Formula: C28H36N6O2S
Exact Mass: 520.2620
Molecular Weight: 520.70
Elemental Analysis: C, 64.59; H, 6.97; N, 16.14; O, 6.15; S, 6.16
The following data is based on the product molecular weight 520.70 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 |
