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MRTX9768

Catalog No. T9575 CAS 2629314-68-5

MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.

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MRTX9768, CAS 2629314-68-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 338.00
5 mg	In stock	$ 713.00
10 mg	In stock	$ 1,130.00
25 mg	In stock	$ 1,690.00
50 mg	In stock	$ 2,270.00
100 mg	In stock	$ 2,970.00

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Purity: 98.48%

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Description	MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
Targets&IC50	Cell proliferation:11 nM(HCT116 MTAP-del cells), Cell proliferation:861 nM(HCT116 MTAP-WT cells), SDMA:3 nM(HCT116 MTAP-del cells), SDMA:544 nM(HCT116 MTAP-WT cells)
In vitro	MRTX-9768, a potent inhibitor of 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).
In vivo	In xenograft studies, oral administration of MRTX-9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1].

Molecular Weight	424.43
Formula	C24H17FN6O
CAS No.	2629314-68-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35 mg/ml(82.46 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Orally Active Compound Library Bioactive Compounds Library Max Reprogramming Compound Library Histone Modification Compound Library Preclinical Compound Library Epigenetics Compound Library Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

MRTX9768 2629314-68-5 Chromatin/Epigenetic Histone Methyltransferase SDMA toxicity glioblastoma orally low Inhibitor hematological MTAP CDKN2A inhibit anticancer PRMT5-MTA MRTX-9768 MRTX 9768 inhibitor

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