MRTX1719 free base · Synonyms: (R)-MRTX-1719 | R-MRTX-1719

MRTX1719 is a synthetic lethal inhibitor of the PRMT5/MTA complex.

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

Target Histone Methyltransferase

Research area Cancer

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Data Sheet SDS COA

MRTX1719 structure

CAS No.: 2630904-45-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 550.00	BP-02037-100mg	In stock	Get quote
250 mg	USD 1,050.00	BP-02037-250mg	In stock	Get quote
500 mg	USD 1,600.00	BP-02037-500mg	In stock	Get quote
1 g	USD 2,650.00	BP-02037-1g	In stock	Get quote
2 g	USD 4,100.00	BP-02037-2g	In stock	Get quote

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Description

MRTX1719 is a synthetic lethal inhibitor of the PRMT5/MTA complex and selectively inhibits PRMT5 activity.

Biological activity

In Vitro Navlimetostat (10 day) inhibits the PRMT5 activity and in MTAP-deleted HCT116 cells not wild type cells, with the IC50 of 8 nM[1]. Navlimetostat (10 day) inhibits the cell viability of MTAP del HCT116 cells with an IC50 value of 12 nM and parental HCT116 cells with an IC50 value of 890 nM. In Vivo Navlimetostat (12.5-100 mg/kg/d for p.o., 21 day) reduces the tumor growth in Lu-99 orthotopic xenograft tumor models.

Identifiers

SMILES: CN1N=CC(C2=CC=C(C(NN=C3CN)=O)C3=C2)=[C@]1[C@]4=C(C#N)C(OC5CC5)=CC(Cl)=C4F
InChIKey: BZKIOORWZAXIBA-UHFFFAOYSA-N

Specifications

MW (average): 464.8790
Formula: C₂₃H₁₈ClFN₆O₂
CAS No.: 2630904-45-7
Physical state: Solid
Color: White to light yellow
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 100 mg/mL

Documents

References

[1]. Lars D Engstrom, et al. MRTX1719 is an MTA-cooperative PRMT5 inhibitor that exhibits synthetic lethality in preclinical models and patients with MTAP deleted cancer. Cancer Discov. 2023 Aug 8;CD-23-0669.

[2]. Christopher R Smith, et al. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers. J Med Chem. 2022 Feb 10;65(3):1749-1766.

Same target

Search Histone Methyltransferase

Same research area

Search Cancer