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Formula | C20H19BrN4O3 |
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Molecular Weight | 443.29 | CAS No. | 781661-94-7 | |
Solubility (25°C)* | In vitro | Water | 89 mg/mL (200.77 mM) | |
DMSO | 60 mg/mL (135.35 mM) | |||
Ethanol | 9 mg/mL (20.3 mM) | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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] |
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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] |
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Data from [Clin Cancer Res, 2013, 19, 5591-601]
Data from [Leukemia, 2012, 26, 623-632]
Data from [Leukemia, 2012, 26, 623-632]
Data from [Proc Natl Acad Sci U S A, 2012, 109, 600-5]
Bivalent chromatin accommodates survivin and BRG1/SWI complex to activate DNA damage response in CD4+ cells [ Cell Commun Signal, 2024, 22(1):440] | PubMed: 39261837 |
Exploring effective biomarkers and potential immune related gene in small cell lung cancer [ Sci Rep, 2024, 14(1):7604] | PubMed: 38556560 |
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 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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