Eribulin

Eribulin is an inhibitor of microtubule assembly and a derivative of the marine sponge macrolide halichondrin B. It inhibits the proliferation of U937 human lymphoma cells, as well as induces cell cycle arrest at the G2/M phase and, subsequently, apoptosis in the same cells when used at a concentration of 100 nM. Eribulin (1.5 mg/kg per week) reduces tumor growth in a patient-derived xenograft (PDX) mouse model of cutaneous squamous cell carcinoma. It also reduces tumor growth and increases survival in an intracerebral U87MG mouse xenograft model of glioblastoma when administered at a dose of 0.5 mg/kg three times per week. Formulations containing eribulin have been used in the treatment of metastatic breast cancer.Formal Name: (2R,3R,3aS,7R,8aS,9S,10aR,11S,12R,13aR,13bS,15S,18S,21S,24S,26R,28R,29aS)-2-[(2S)-3-amino-2-hydroxypropyl]hexacosahydro-3-methoxy-26-methyl-20,27-bis(methylene)-11,15:18,21:24,28-triepoxy-7,9-ethano-12,15-methano-9H,15H-furo[3,2-i]furo[2',3':5,6]pyrano[4,3-b][1,4]dioxacyclopentacosin-5(4H)-one. CAS Number: 253128-41-5. Synonyms: B1939, E7389, ER 086526. Molecular Formula: C40H59NO11. Formula Weight: 729.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Chloroform: Sparingly soluble: 1-10 mg/ml, Methanol: Slightly soluble: 0.1-1 mg/ml. SMILES: [H][C@@]1([C@H](O2)[C@@](O[C@@]3([H])[C@]4([H])O[C@]25C3)([H])[C@@]4([H])O6)[C@]6([H])CC[C@@](CC(C[C@]7([H])[C@@H](OC)[C@@H](C[C@H](O)CN)O[C@@]7([H])C[C@]8([H])C([C@H](C)C[C@]([H])(CC[C@@]9([H])C(C[C@@](CC5)([H])O9)=C)O8)=C)=O)([H])O1. InChi Code: InChI=1S/C40H59NO11/c1-19-11-24-5-7-28-20(2)12-26(45-28)9-10-40-17-33-36(51-40)37-38(50-33)39(52-40)35-29(49-37)8-6-25(47-35)13-22(42)14-27-31(16-30(46-24)21(19)3)48-32(34(27)44-4)15-23(43)18-41/h19,23-39,43H,2-3,5-18,41H2,1,4H3/t19-,23+,24+,25-,26+,. InChi Key: UFNVPOGXISZXJD-JBQZKEIOSA-N.