Description
An estrogen sulfamate with anticancer activities; inhibits steroid sulfatase (IC50s = 39 and 0.5 nM in placental microsomes and MCF-7 cancer cells, respectively); binds to carbonic anhydrase IX and II (Kis = 70 and 270 nM, respectively); inhibits bovine brain tubulin assembly in a cell-free assay (IC50 = 2.2 µM) and tubule formation in HUVECs at 50 and 100 nM; 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); reduces angiogenesis in a Matrigel™ plug assay in mice and tumor growth in MCF-7 and MDA-MB-231 mouse xenograft models at 20 mg/kg
Formal name: 2-methoxy-estra-1,3,5(10)-triene-3,17β-diol, disulfamate
Synonyms: 2-MeOE2bisMATE|2-Methoxyestradiol-bis-sulphamate
Molecular weight: 460.6
CAS: 401600-86-0
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Microtubule Dynamics||Product Type|Biochemicals|Small Molecule Inhibitors|Carbonic Anhydrase||Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Multidrug Resistance||Research Area|Cell Biology|Cytoskeleton & Motor Proteins
