MRTX9768 free base · Synonyms: MRTX-9768 · MRTX 9768

MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex 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

MRTX9768 structure

CAS No.: 2629314-68-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 mg	USD 450.00	BP-02036-10mg	In stock	Get quote
25 mg	USD 675.00	BP-02036-25mg	In stock	Get quote
50 mg	USD 945.00	BP-02036-50mg	In stock	Get quote
100 mg	USD 1,325.00	BP-02036-100mg	In stock	Get quote
250 mg	USD 1,988.00	BP-02036-250mg	In stock	Get quote
500 mg	Inquire	BP-02036-500mg	In stock	Inquire
1 g	Inquire	BP-02036-1g	In stock	Inquire

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Description

MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.

Biological activity

In Vitro MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM). MRTX9768 (0-250 nM) results in LU99 SDMA inhibition maintaining after 3-hr drug treatment followed by 4-day washout (exhibiting tight binding and prolonged PRMT5 MTA occupancy). In Vivo In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow. MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors (such as glioblastoma). MRTX9768 (PO dose 30 mg/kg in CD-1 mouse and beagle dog, 10 mg/kg in cynomolgus monkey) has a favorable ADME profile (>50% bioavailability in mice and dogs, moderate to high clearance, No changes in RBC parameters when administered well above efficacious concentrations (1000 mg/kg)). MRTX9768 (100 mg/kg, orally, BID, 6/21 days) results in SDMA inhibition maintaining 3 days after dosing is stopped.

Identifiers

SMILES: FC1=C(C(C#N)=C2C=CC=CC2=C1)C3=C(C=NN3C)C4=CC=C(C5=C4)C(NN=C5CN)=O
InChIKey: BPTYWAYMKBEXES-UHFFFAOYSA-N

Specifications

MW (average): 424.4298
Formula: C₂₄H₁₇FN₆O
CAS No.: 2629314-68-5
Physical state: Solid
Color: White to light brown
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°C, protect from light; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 50 mg/mL

Documents

References

[1]. Christopher R. Smith, et al. Abstract LB003: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors. Cancer Res 1 July 2021; 81 (13_Supplement): LB003.

[2]. Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252.

[3]. Matthew A. Marx, et al. Fragment-based discovery of MRTX9768, a synthetic lethal- based inhibitor designed to bind the PRMT5•MTA complex and selectively target MTAPDEL tumors. AACR ANNUAL MEETING 2021:APRIL 10-15, 2021 AND MAY 17-21, 2021.

Same target

Search Histone Methyltransferase

Same research area

Search Cancer