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您的检索式：作者名="Krista Menard"
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| 1 | Tissue distribution and tumor uptake of folate receptor–targeted epothilone folate conjugate,BMS-753493,in CD2F1 mice after systemic administration显示文摘To assess targeting of an epothilone folate conjugate(BMS-753493) to the folate receptor(FR)-overexpressed tumor in mice bearing both FRt and FR– tumors,a series of experiments were conducted by quantitative whole-body autoradiography(QWBA) and LC–MS/MS following i.v.administration of BMS-753493 or its active moiety,BMS-748285 in mice bearing FRt(98M109) and FR–(M109) tumors.QWBA showed [3H]BMS-753493–derived radioactivity was extensively distributed to various tissues.The FR over-expressing 98M109 tumors showed consistently higher level of radioactivity than FR-negative tumors(i.e.,M109 tumors) up to 48 h post dose of [3H]BMS-753493,despite the magnitude of difference between the tumors is relatively small(generally 3 5-fold).The radioactivity level in 98M109 tumors was 2 12-fold of normal tissues except intestine/content at 48 h post dose.No selective radioactivity uptake into 98M109 tumors over M109 or normal tissues was observed after i.v.administration of the active epothilone,[3H]BMS-748285.LC–MS/MS measurements demonstrated that the concentrations of BMS-748285,presumably from hydrolysis of the folate conjugate,in 98M109 tumors were greater than those in M109 tumors after i.v.administration of BMS-753493(2–3-fold) whereas no differential uptake in the tumors following BMS-748285 administration.Those data were consistent with radioactivity determinations.Those results demonstrated that the folate conjugation in BMS-753493 enabled moderately preferential distribution of the active epothilone to FR overexpressing 98M109 tumors,thereby supporting targeted delivery of cytotoxics through the folate receptor. | Hong Shen Lifei Wang Weiqi Chen Krista Menard Yang Hong Yuan Tian Samuel J.Bonacorsi W.Griffith Humphreys Francis Y.Lee Jinping Gan | 2016 | Acta Pharmaceutica Sinica B2016，6，5： | 3 |
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