An estrogen sulfamate with anticancer activities; inhibits steroid sulfatase (IC50s = 39 and 0.5 nM in placental microsomes and MCF-7 cancer cells

STX140 – 5 mg

Brand:
Cayman
CAS:
401600-86-0
Storage:
-20
UN-No:
Non-Hazardous - /

STX140 is an estrogen sulfamate with anticancer activities.{48571} 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).{35834} 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.{48572,48573} 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).{48574,48575} It reduces angiogenesis in a Matrigel™ 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.{48576,48575}  

 

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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

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