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化学情報
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Synonyms | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C20H19BrN4O3 |
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| 分子量 | 443.29 | CAS No. | 781661-94-7 | |
| Solubility (25°C)* | 体外 | Water | 89 mg/mL (200.77 mM) | |
| DMSO | 55 mg/mL (124.07 mM) | |||
| Ethanol | 6 mg/mL (13.53 mM) | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2. |
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| in vitro | YM155 is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. YM155 significantly inhibits endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 through transcriptional inhibition of the survivin gene promoter. On the contrary YM155 shows no sufficient effect on protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at 100 nM. YM155 indicates great apoptosis in human cancer cell lines including PC-3 and PPC-1 with a concomitant increase in caspase-3 activity. YM155 potently inhibits human cancer cell lines (mutated or truncated p53) including PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50 from 2.3 to 11 nM, respectively. [1] YM155 increases the sensitivity of NSCLC cells to γ-radiation. The combination of YM155 and γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA. [2] |
| in vivo | YM155 completely inhibits the tumor growth of PC-3 s.c. xenografted prostate tumors at doses of 3 and 10 mg/kg, without body weight loss and blood cell count decrease. Pharmacokinetic analysis shows that YM155 is highly distributed to tumor tissue. Moreover, YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. [1] The combination therapy with YM155 and γ-radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice. [2] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Promoter-luciferase reporter assay | |
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| A 2,767-bp sequence of human survivin gene promoter is isolated from human genomic DNA by PCR using Pyrobest polymerase and the following primers: 5 | ||
| 細胞アッセイ | 細胞株 | Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375) |
| 濃度 | ~ 100 nM | |
| 反応時間 | 48 hours | |
| 実験の流れ | Cells are seeded in 96-well plates at a density of 5-40 × 103. YM155 is dissolved in DMSO and added to cells for 48 hours. Then the cell count is determined by sulforhodamine B assay. |
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| 動物実験 | 動物モデル | PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu) |
| 投薬量 | 5 mg/kg | |
| 投与方法 | Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump | |
参考
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カスタマーフィードバック
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Data from [Clin Cancer Res, 2013, 19, 5591-601]
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Data from [Leukemia, 2012, 26, 623-632]
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Data from [Leukemia, 2012, 26, 623-632]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| TP53RK Drives the Progression of Chronic Kidney Disease by Phosphorylating Birc5 [ Adv Sci (Weinh), 2023, 10(25):e2301753] | PubMed: 37382161 |
| Fusion-negative rhabdomyosarcoma 3D organoids to predict effective drug combinations: A proof-of-concept on cell death inducers [ Cell Rep Med, 2023, 4(12):101339] | PubMed: 38118405 |
| CBX5 loss drives EGFR inhibitor resistance and results in therapeutically actionable vulnerabilities in lung cancer [ Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120] | PubMed: 36652476 |
| FAP is critical for ovarian cancer cell survival by sustaining NF-κB activation through recruitment of PRKDC in lipid rafts [ Cancer Gene Ther, 2023, 30(4):608-621] | PubMed: 36494579 |
| Survivin prevents the polycomb repressor complex 2 from methylating histone 3 lysine 27 [ iScience, 2023, 26(7):106976] | PubMed: 37534134 |
| Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] | PubMed: 35868306 |
| Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] | PubMed: 35704690 |
| Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] | PubMed: 35332332 |
| Effects of YM155 on the proliferation and apoptosis of pulmonary artery smooth muscle cells in a rat model of high pulmonary blood flow-induced pulmonary arterial hypertension [ Clin Exp Hypertens, 2022, 44(5):470-479] | PubMed: 35507763 |
| CDK/cyclin dependencies define extreme cancer cell-cycle heterogeneity and collateral vulnerabilities [ Cell Rep, 2022, 38(9):110448] | PubMed: 35235778 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。