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SPIRO PHARMA |
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eric_feng1954@126.com |
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Musechem |
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1-(2-Methoxyethyl)-2-Methyl-4,9-dioxo-3-(pyrazin-2-ylMethyl)-4,9-dihydro-1H-naphtho[2,3-d]iMidazol-3-iuM chloride manufacturers
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| | 1-(2-Methoxyethyl)-2-Methyl-4,9-dioxo-3-(pyrazin-2-ylMethyl)-4,9-dihydro-1H-naphtho[2,3-d]iMidazol-3-iuM chloride Basic information |
| | 1-(2-Methoxyethyl)-2-Methyl-4,9-dioxo-3-(pyrazin-2-ylMethyl)-4,9-dihydro-1H-naphtho[2,3-d]iMidazol-3-iuM chloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | ≥19.45 mg/mL in DMSO; ≥4.34 mg/mL in EtOH with gentle warming and ultrasonic; ≥48.1 mg/mL in H2O with ultrasonic | | form | solid | | color | Light brown to brown |
| | 1-(2-Methoxyethyl)-2-Methyl-4,9-dioxo-3-(pyrazin-2-ylMethyl)-4,9-dihydro-1H-naphtho[2,3-d]iMidazol-3-iuM chloride Usage And Synthesis |
| Uses | Sepantronium hydrochloride (YM-155 hydrochloride) is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity[1]. | | in vivo | Sepantronium bromide (YM155; 3 and 10 mg/kg) inhibits the tumor growth in PC-3 xenografts, without obvious body weight loss and blood cell count decrease. Sepantronium bromide is highly distributed to tumor tissue in vivo. Sepantronium bromide shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts[1].
Sepantronium bromide (YM155) in combination with γ-radiation shows potent antitumor activity against H460 or Calu6 xenografts in nude mice[2].
In this orthotopic renal and metastatic lung tumors models, Sepantronium bromide (YM-155) and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images[3]. | | target | survivin | | References | [1] Nakahara T, et al. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts. Cancer Res. 2007 Sep 1;67(17):8014-21. DOI:10.1158/0008-5472.CAN-07-1343 [2] Iisa T, et al. Radiosensitizing effect of YM155, a novel small-molecule survivin suppressant, in non-small cell lung cancer cell lines. Clin Cancer Res. 2008 Oct 15;14(20):6496-504. DOI:10.1158/1078-0432.CCR-08-0468 [3] Guo K, et al. A combination of YM-155, a small molecule survivin inhibitor, and IL-2 potently suppresses renal cell carcinoma in murine model. Oncotarget. 2015 Aug 28;6(25):21137-47. DOI:10.18632/oncotarget.4121 |
| | 1-(2-Methoxyethyl)-2-Methyl-4,9-dioxo-3-(pyrazin-2-ylMethyl)-4,9-dihydro-1H-naphtho[2,3-d]iMidazol-3-iuM chloride Preparation Products And Raw materials |
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