| Identification | Back Directory | [Name]
N-(6-amino-5-ethylpyridin-3-yl)-2-((2R,5S)-5-methyl-2-(2-(1-methylpiperidin-4-yl)benzo[d]thiazol-5-yl)piperidin-1-yl)-2-oxoacetamide | [CAS]
2760483-96-1 | [Synonyms]
N-(6-amino-5-ethylpyridin-3-yl)-2-((2R,5S)-5-methyl-2-(2-(1-methylpiperidin-4-yl)benzo[d]thiazol-5-yl)piperidin-1-yl)-2-oxoacetamide | [Molecular Formula]
C28H36N6O2S | [MOL File]
2760483-96-1.mol | [Molecular Weight]
520.69 |
| Chemical Properties | Back Directory | [density ]
1.266±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
11.337±0.70(predicted) | [color ]
White to off-white | [InChIKey]
DHAGMIPSRSPWSH-GAJHUEQPSA-N | [SMILES]
C(N1C[C@H](CC[C@@H]1C1=CC=C2SC(C3CCN(CC3)C)=NC2=C1)C)(=O)C(=O)NC1=CN=C(C(=C1)CC)N |
| Hazard Information | Back Directory | [Uses]
TNG-462 is an orally active and selective PRMT5 inhibitor with anti-tumor activity against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation cancers[1][2]. | [in vivo]
TNG-462 (40, 100 mg/kg; once daily (100 mg/kg) or b.i.d (40 mg/kg); 21 days; p.o.) has anti-tumor activity in a xenograft mouse model derived from MTAP deficient cell lines[1].
TNG-462 (30 mg/kg; twice daily; 5 weeks; p.o.) in combination with osimertinib (EGFR inhibitor) (HY-15772) (1 mg/kg; once daily; 5 weeks) has synergistic anti-tumor activity in MTAP-deficient cell line-derived xenograft mouse model[1]. | Animal Model: | LU99 MTAP-null cell line-derived xenograft mice model[1]. | | Dosage: | 40, 100 mg/kg | | Administration: | Oral gavage (p.o.); once daily (100 mg/kg) or b.i.d (40 mg/kg); 21 days | | Result: | Inhibited the growth of tumor volume. |
| [References]
[1] Briggs K, et al. TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted solid tumors[J]. Cancer Research, 2023, 83(7_Supplement): 4970-4970.
[2] Kevin M Cottrell, et al. Piperidin-1- yl-n-pyrydi ne-3-yl-2-oxoacet am ide derivatives useful for the treatment of mtap-deficient and/or mt a-accumulating cancers. Patent WO2022026892A1. |
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