{"product_id":"m17710","title":"PROTAC BRD2\/BRD4 degrader-1","description":"\u003cp style=\"padding-left: 1em;\"\u003ePROTAC BRD2\/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader. PROTAC BRD2\/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2\/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)\/cullin 4A.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 766.82\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C39H38N6O9S\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e N-[4-[[2-(2, 6-dioxopiperidin-3-yl)-1, 3-dioxoisoindol-4-yl]amino]butyl]-3-[6-[(2-methoxyphenyl)sulfonylamino]-1-methyl-2-oxobenzo[cd]indol-4-yl]propanamide\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CN1C2=CC=C(NS(=O)(=O)C3=CC=CC=C3OC)C3=CC(CCC(=O)NCCCCNC4=CC=CC5=C4C(=O)N(C4CCC(=O)NC4=O)C5=O)=CC(C1=O)=C32\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e DCPKSVYPNGBDSB-UHFFFAOYSA-N\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C39H38N6O9S\/c1-44-28-14-13-26(43-55(52,53)31-11-4-3-10-30(31)54-2)24-20-22(21-25(34(24)28)37(44)49)12-16-32(46)41-19-6-5-18-40-27-9-7-8-23-35(27)39(51)45(38(23)50)29-15-17-33(47)42-36(29)48\/h3-4,7-11,13-14,20-21,29,40,43H,5-6,12,15-19H2,1-2H3,(H,41,46)(H,42,47,48)\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\n\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\n\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\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\n\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\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003ePROTAC BRD2\/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50 value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells. PROTAC BRD2\/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50 value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells. PROTAC BRD2\/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines. PROTAC BRD2\/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI50 values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells. PROTAC BRD2\/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC50: 0.081 μM), colon cancer (colo-205 IC50: 0.1557 μM) and thyroid cancer(TT IC50: 0.037451 μM).\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M17710-C \/ Contact sales@xcessbio.com for quotation","offer_id":39512881889419,"sku":"0","price":100.0,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/files\/1687934562984_1.png?v=1687934585","url":"https:\/\/www.xcessbio.com\/products\/m17710","provider":"Xcess Biosciences","version":"1.0","type":"link"}