STX140

STX140 is an estrogen sulfamate with anticancer activities. It inhibits steroid sulfatase with IC50 values of 39 and 0.5 nM in placental microsomes and MCF-7 cancer cells, respectively. STX140 also binds to carbonic anhydrase IX and II (Kis = 70 and 270 nM, respectively). It inhibits bovine brain tubulin assembly in a cell-free assay (IC50 = 2.2 µM) and tubule formation in human umbilical vein epithelial cells (HUVECs) when used at concentrations of 50 and 100 nM. STX140 inhibits proliferation of LNCaP, PC3, and MDA-MB-231 cancer cells, as well as wild-type A2780 cancer cells and adriamycin- and cisplatin-resistant A2780 cancer cells (IC50s = 530, 400, 618, 330, 870, and 380 nM, respectively). It reduces angiogenesis in a Matrigel(TM) plug assay in mice and tumor growth in MCF-7 and MDA-MB-231 mouse xenograft models when used at a dose of 20 mg/kg.Formal Name: 2-methoxy-estra-1,3,5(10)-triene-3,17beta-diol, disulfamate. CAS Number: 401600-86-0. Synonyms: 2-Methoxyestradiol-bis-sulphamate. Molecular Formula: C19H28N2O7S2. Formula Weight: 460.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:7): 0.1 mg/ml, DMSO: 25 mg/ml, Ethanol: 14 mg/ml. SMILES: COC1=C(OS(N)(=O)=O)C=C(CC[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4OS(N)(=O)=O)C3=C1. InChi Code: InChI=1S/C19H28N2O7S2/c1-19-8-7-12-13(15(19)5-6-18(19)28-30(21,24)25)4-3-11-9-17(27-29(20,22)23)16(26-2)10-14(11)12/h9-10,12-13,15,18H,3-8H2,1-2H3,(H2,20,22,23)(H2,21,24,25)/t12-,13+,15-,18-,19-/m0/s1. InChi Key: AQSNIXKAKUZPSI-SSTWWWIQSA-N.