{"product_id":"m12132","title":"SJG-136","description":"\u003cp style=\"padding-left:1em;\"\u003eSJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 232931-57-6\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 556.61\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C31H32N4O6\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eSynonym:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eNSC-694501\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e (7S)-13-methoxy-12-(3-{[(7S)-13-methoxy-5-methylidene-2-oxo-3, 9-diazatricyclo[8.4.0.0, ]tetradeca-1(14), 8, 10, 12-tetraen-12-yl]oxy}propoxy)-5-methylidene-3, 9-diazatricyclo[8.4.0.0, ]tetradeca-1(14), 8, 10, 12-tetraen-2-one\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e COC1=CC2=C(C=C1OCCCOC1=CC3N=C[C@@H]4CC(=C)CN4C(=O)C=3C=C1OC)N=C[C@@H]1CC(=C)CN1C2=O\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e RWZVMMQNDHPRQD-SFTDATJTSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C31H32N4O6\/c1-18-8-20-14-32-24-12-28(26(38-3)10-22(24)30(36)34(20)16-18)40-6-5-7-41-29-13-25-23(11-27(29)39-4)31(37)35-17-19(2)9-21(35)15-33-25\/h10-15,20-21H,1-2,5-9,16-17H2,3-4H3\/t20-,21-\/m0\/s1\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 : 33.33 mg\/mL (59.88 mM; Need ultrasonic)\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 ≥360 days 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;\"\u003eSJG-136 (dimer 5) is a DNA cross-linking agent, with an XL50 (concentration of agent required for 50% cross-linking of pBR322 DNA) of 45 nM for pBR322 DNA. SJG-136 is cytotoxic to ovarian cell lines, such as A2780 (IC50, 22.5 pM), A2780cisR (IC50, 24 pM), CH1 (IC50, 0.12 nM), CH1cisR (IC50, 0.6 nM), and SKOV-3 (IC50, 9.1 nM). SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI50 values ranging from 0.33 - \u0026gt;100 nM after a 1 h exposure, and \u0026lt;0.03 - 17.33 nM following continuous exposure.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eSJG-136 shows more potent antitumor effect against CMeC-1 tumour at 0.30 mg\/kg than 0.15 mg\/kg either as a single dose or administered once a week for three weeks via dosed intravenously in mice. SJG-136-induced H2AX phosphorylation shows good correspondence, but less sensitivity, than measurement of foci.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eReferences:\u003c\/strong\u003e\u003c\/p\u003e\u003col style=\"padding-left:1em;\"\u003e\n\u003cli\u003eGregson SJ, et al. Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity. J Med Chem. 2001 Mar 1;44(5):737-48.\u003c\/li\u003e\n\u003cli\u003eMellinas-Gomez M, et al. Activity of the DNA minor groove cross-linking agent SG2000 (SJG-136) against canine tumours. BMC Vet Res. 2015 Aug 19;11:215.\u003c\/li\u003e\n\u003c\/ol\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":"M12132-2 \/ 2mg solid","offer_id":39404978569355,"sku":"","price":570.0,"currency_code":"USD","in_stock":true},{"title":"M12132-10 \/ 10mg solid","offer_id":39404978602123,"sku":"","price":2280.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/products\/M12132_1625112714.gif?v=1626949080","url":"https:\/\/www.xcessbio.com\/products\/m12132","provider":"Xcess Biosciences","version":"1.0","type":"link"}