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MRTX1719

Chemical Structure : MRTX1719

CAS No.: 2630904-45-7

MRTX1719 (MRTX-1719)

Catalog No.: PC-72393Not For Human Use, Lab Use Only.

MRTX1719 (MRTX-1719) is a potent, selective binder to the PRMT5-MTA complex, selectively inhibits PRMT5 activity in MTAP-deleted cells (HCT116 MTAP-deleted IC50=12 nM) compared to MTAP-wild-type cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MRTX1719 (MRTX-1719) is a potent, selective binder to the PRMT5-MTA complex, selectively inhibits PRMT5 activity in MTAP-deleted cells (HCT116 MTAP-deleted IC50=12 nM) compared to MTAP-wild-type cells.
MRTX1719 demonstrated dose-dependent inhibition of PRMT5-dependent symmetric dimethylarginine protein modification in MTAP-deleted tumors that correlated with antitumor activity in tumor xenograft-bearing mice.
MRTX1719 is a novel synthetically lethal drug target for the treatment of MTAP-deleted cancers.

Physicochemical Properties

M.Wt 464.885
Formula C23H18ClFN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile

References

1. Christopher R Smith, et al. J Med Chem. 2022 Feb 10;65(3):1749-1766.

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