Phenoxodiol (Synonyms: Haginin E, Phenoxodiol) |
| رقم الكتالوجGC36895 |
Phenoxodiol (Idronoxil) ، وهو نظير اصطناعي لـ Genestein ، ينشط نظام mitochondrial caspase ، ويمنع XIAP (مثبط موت الخلايا المبرمج) ، ويحسس الخلايا السرطانية لموت الخلايا المبرمج Fasيثبط الفينوكسوديول أيضًا DNA topoisomerase II من خلال تثبيت المركب القابل للانقساميحث الفينوكسوديول على إيقاف دورة الخلية في طور G1 / S من دورة الخلية وينظم p21WAF1 بطريقة مستقلة عن p53
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Cas No.: 81267-65-4
Sample solution is provided at 25 µL, 10mM.
Phenoxodiol is an isoflavone derivative with antitumor activity[1]. Phenoxodiol can induce G1 arrest in cells through p53-independent induction of p21WAF1/CIP1, resulting in loss of cyclin-dependent kinase 2 activity[2]. Phenoxodiol can induce apoptosis and target plasma membrane electron transport (PMET)[3].
In vitro, treatment of prostate cancer cell lines (LNCaP, DU145 and PC3 cells) with Phenoxodiol (10, 30μM) for 24h and 48h upregulated the expression of p21WAF1 in all cell lines and induced cell cycle arrest at the G1/S phase[4]. Pretreatment of epithelial ovarian cancer (EOC) cells with Phenoxodiol (10μg/mL) for 2h significantly reduced cell viability and enhanced the sensitivity of cells to chemotherapy[5]. Phenoxodiol (0-10μg/mL) treatment of LNCaP cells for 24h significantly inhibited cell proliferation and reduced colony formation in a dose-dependent manner[6].
In vivo, Phenoxodiol (10mg/kg) was orally treated for 16 days in mice with U2OS cell xenografts. When combined with Doxorubicin (1mg/kg, i.p.), it was able to significantly inhibit tumor growth. The tumor growth inhibition effect of the group receiving only single treatment was weak[7].
References:
[1] Choueiri T K, Wesolowski R, Mekhail T M. Phenoxodiol: isoflavone analog with antineoplastic activity[J]. Current oncology reports, 2006, 8: 104-107.
[2] Aguero M F, Facchinetti M M, Sheleg Z, et al. Phenoxodiol, a novel isoflavone, induces G1 arrest by specific loss in cyclin-dependent kinase 2 activity by p53-independent induction of p21WAF1/CIP1[J]. Cancer research, 2005, 65(8): 3364-3373.
[3] Herst P M, Petersen T, Jerram P, et al. The antiproliferative effects of phenoxodiol are associated with inhibition of plasma membrane electron transport in tumour cell lines and primary immune cells[J]. Biochemical pharmacology, 2007, 74(11): 1587-1595.
[4] Mahoney S, Arfuso F, Millward M, et al. The effects of phenoxodiol on the cell cycle of prostate cancer cell lines[J]. Cancer cell international, 2014, 14: 1-12.
[5] Alvero A B, O'Malley D, Brown D, et al. Molecular mechanism of phenoxodiol‐induced apoptosis in ovarian carcinoma cells[J]. Cancer: Interdisciplinary International Journal of the American Cancer Society, 2006, 106(3): 599-608.
[6] Yao C, Wu S, Li D, et al. Co-administration phenoxodiol with doxorubicin synergistically inhibit the activity of sphingosine kinase-1 (SphK1), a potential oncogene of osteosarcoma, to suppress osteosarcoma cell growth both in vivo and in vitro[J]. Molecular oncology, 2012, 6(4): 392-404.
[7] Aguero M F, Venero M, Brown D M, et al. Phenoxodiol inhibits growth of metastatic prostate cancer cells[J]. The Prostate, 2010, 70(11): 1211-1221.
| Cell experiment [1]: | |
Cell lines | LNCaP、DU145、PC3 cells |
Preparation Method | Cells were cultured in vitro, and then treated with Phenoxodiol (10μM and 30μM) for 24 and 48h. The expression of cell cycle genes p21WAF1, c-Myc, Cyclin-D1, and Ki-67 was investigated by Real Time PCR. |
Reaction Conditions | 10, 30μM; 24, 48h |
Applications | Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle, with the resultant arrest due to the upregulation of p21WAF1 in all the cell lines in response to treatment. |
| Animal experiment [2]: | |
Animal models | CB.17 severe combined immuno-deficient (SCID) male mice |
Preparation Method | Mice was injected subcutaneously (s.c.) into the right flank with 1.5×106 U2OS cells in 0.1 ml DMEM. When the right flank xenografts were established at about 500mm3, the animals (5 mice per group) were treated daily with Doxorubicin (1mg/kg, i.p.), Phenoxodiol (10mg/kg, p.o.) or both for 16 days before sacrifice. Xenograft diameters were measured every 4 days using calipers. |
Dosage form | 10mg/kg/day for 16 days; p.o. |
Applications | Only group that received both Phenoxodiol and Doxorubicin showed a significant reduced tumor growth. The group that received either single treatment showed slight anti-tumor growth effect as compared to vehicle controls. |
References: | |
| Cas No. | 81267-65-4 | SDF | |
| المرادفات | Haginin E, Phenoxodiol | ||
| Canonical SMILES | OC1=CC=C2C=C(C3=CC=C(O)C=C3)COC2=C1 | ||
| Formula | C15H12O3 | M.Wt | 240.25 |
| الذوبان | DMSO: ≥ 100 mg/mL (416.23 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1623 mL | 20.8117 mL | 41.6233 mL |
| 5 mM | 832.5 μL | 4.1623 mL | 8.3247 mL |
| 10 mM | 416.2 μL | 2.0812 mL | 4.1623 mL |
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- Purity: >98.00%
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