Formulation: A solid
Formal Name: 3,11-difluorohydro-6,8,13-trimethyl-quino[4,3,2-kl]acridinium, methyl sulfate
Purity: ≥98%
Formula Markup: C22H17F2N2 • CH3SO4
Formula Weight: 458,5
Shelf life (days): 1460
CAS Number: 390362-78-4
Notes: RHPS4 is a telomerase inhibitor (IC50 = 0.33 µM).{61866} It is a ligand for the guanine quadruplex (G-quadruplex), a four-stranded DNA secondary structure formed from G-rich DNA sequences, that intercalates and stabilizes the G-quadruplex, which inhibits the activity of telomerase.{61866,61867} RHPS4 (1 µM) induces phosphorylation of H2AX on telomeres, indicating telomeric DNA damage, in BJ fibroblasts expressing human telomerase.{61868} It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI50 = 13.18 µM), as well as induces cell cycle arrest at the S-G2/M and apoptosis in M14 melanoma cells when used at concentrations ranging from 0.5 to 10 µM.{61869,61870} RHPS4 (10 mg/kg) reduces tumor growth in several mouse xenograft models, including melanoma, lung, breast, and colon cancer models.{61871}
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