{"product_id":"m34869","title":"MRTX9768","description":"\u003cp style=\"padding-left:1em;\"\u003eMRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 2629314-68-5\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 424.43\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C24H17FN6O\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e 2-{4-[4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-1H-pyrazol-5-yl}-3-fluoronaphthalene-1-carbonitrile\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CN1N=CC(=C1C1C(F)=CC2C=CC=CC=2C=1C#N)C1=CC2C(CN)=NNC(=O)C=2C=C1\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e BPTYWAYMKBEXES-UHFFFAOYSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C24H17FN6O\/c1-31-23(22-18(10-26)15-5-3-2-4-13(15)9-20(22)25)19(12-28-31)14-6-7-16-17(8-14)21(11-27)29-30-24(16)32\/h2-9,12H,11,27H2,1H3,(H,30,32)\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSolubility:\u003c\/strong\u003e DMSO : 50 mg\/mL (117.81 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO).\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eMRTX9768 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).\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eIn 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 (\u0026gt;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.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M34869-C \/ Contact sales@xcessbio.com for quotation","offer_id":43180866011275,"sku":null,"price":100.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/files\/M34869_1743256167.gif?v=1743256167","url":"https:\/\/www.xcessbio.com\/products\/m34869","provider":"Xcess Biosciences","version":"1.0","type":"link"}