TNG462 free base · Synonyms: TNG-462 · TNG 462

TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor.

For research use only. Not for human or veterinary use.

Target Histone Methyltransferase

Research area Cancer

Purity 98+% Stock Inquire

Data Sheet SDS COA

TNG462 structure

CAS No.: 2760483-96-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 885.00	BP-02049-25mg	In stock	Get quote
100 mg	USD 1,800.00	BP-02049-100mg	In stock	Get quote
500 mg	USD 3,900.00	BP-02049-500mg	In stock	Get quote
1 g	Inquire	BP-02049-1g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted solid tumors.

Biological activity

In Vitro TNG-462 (0-1 μM) exhibits selectivity and inhibition of cell viability in MTAP deficient tumor cells (NSCLC, PDAC, bladder, hematological malignancies), with IC50values less than 1 μM. 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. 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.

Identifiers

SMILES: O=C(NC1=CC(CC)=C(N)N=C1)C(N2[C@@H](C3=CC=C(SC(C4CCN(C)CC4)=N5)C5=C3)CC[C@H](C)C2)=O
InChIKey: DHAGMIPSRSPWSH-GAJHUEQPSA-N

Specifications

MW (average): 520.6890
Formula: C₂₈H₃₆N₆O₂S
CAS No.: 2760483-96-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 100 mg/mL

Documents

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.

Same target

Search Histone Methyltransferase

Same research area

Search Cancer