| Name | TNG-462 |
| Description | TNG-462 is a potent and selective PRMT5 inhibitor with antitumor activity and oral activity, primarily for the treatment of methylthioadenosine phosphorylase (MTAP)-deficient and/or methylthioadenosine (MTA)-accumulating cancers (e.g., non-small-cell lung cancer, pancreatic cancer, bladder cancer, and hematologic malignancies). |
| In vitro | Methods: Tumor cells (NSCLC, PDAC, bladder, hematological malignancies) deficient in MTAP were treated with TNG-462 (0-1 μM) and cell viability was measured.
Results: TNG-462 selectively inhibited cell viability with an IC50 value of less than 1 μM. [2] |
| In vivo | Methods: TNG-462 (40 mg twice a day; 100 mg/kg twice a day, orally, for 21 days) was used to treat a xenograft mouse model derived from a MTAP-deficient cell line and observe tumor growth in vivo.
Results: TNG-462 inhibited tumor growth in mice and showed anti-tumor activity. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 80 mg/mL (153.64 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.34 mM), Sonication is recommended.
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| Keywords | HistoneMethyltransferase | Histone Methyltransferase |
| Inhibitors Related | MAK-683 hydrochloride | SNDX-5613 | Tazemetostat | Piribedil | XY1 | UNC 0631 | （Iso）-Flavokawain A | EPZ015666 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Post-Translational Modification Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
