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| Product Name: | STX140 | | Synonyms: | STX140;Estra-1,3,5(10)-triene-3,17-diol, 2-methoxy-, disulfamate, (17β)-;2-methoxy-estra-1,3,5(10)-triene-3,17β-diol, disulfamate;(9Beta,13α,14Beta,17α)-2-Methoxyestra-1,3,5(10)-triene-3,17-diyl disulfamate | | CAS: | 401600-86-0 | | MF: | C19H28N2O7S2 | | MW: | 460.56 | | EINECS: | | | Product Categories: | | | Mol File: | 401600-86-0.mol |  |
| | STX140 Chemical Properties |
| Boiling point | 644.8±65.0 °C(Predicted) | | density | 1.47±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:7): 0.1 mg/ml; DMSO: 25 mg/ml; Ethanol: 14 mg/ml | | form | A crystalline solid | | pka | 8.81±0.70(Predicted) |
| | STX140 Usage And Synthesis |
| Description | 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™ 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. | | Uses | STX140 is an orally active microtubule disruptor. STX140 induces apoptosis in the hormone-independent PC-3 prostate cell lines. STX140 has anti-angiogenic and anti-tumour activities[1]. | | in vivo | STX140 (20mg/kg; p.o.; once daily; 60 days) leads to tumour regression and complete responses, which are maintained after the cessation of dosing[1]. | Animal Model: | Male MF-1 nu/nu mice injected with PC-3 cells[1] | | Dosage: | 20mg/kg | | Administration: | p.o.; once daily; 60 days | | Result: | Led to tumour regression and complete responses.
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| | References | [1] S P Newman, et al. The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers. Br J Cancer. 2007 Dec 17;97(12):1673-82. DOI:10.1038/sj.bjc.6604100 |
| | STX140 Preparation Products And Raw materials |
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