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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 2 years

Solubility Information

DMSO: 35 mg/ml(82.46 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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：

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

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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