| Chemical Properties | Back Directory | [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) |
| Hazard Information | Back Directory | [Description]
STX140 is an estrogen sulfamate with anticancer activities.1 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).2 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.3,4 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).5,6 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.7,6 | [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 (20?mg/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: | 20?mg/kg | | Administration: | p.o.; once daily; 60 days | | Result: | Led to tumour regression and complete responses.
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| [storage]
Store at -20°C | [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 |
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