受注:045-509-1970 |
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Synonyms | Nogitecan HCl, SKFS 104864A, NSC 609699 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H23N3O5.HCl |
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分子量 | 457.91 | CAS No. | 119413-54-6 | ||||
Solubility (25°C)* | 体外 | DMSO | 92 mg/mL (200.91 mM) | ||||
Water | 92 mg/mL (200.91 mM) | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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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. |
製品説明 | Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis. |
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in vitro | Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. [1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. [2] |
in vivo | Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. [1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. [2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. [3] |
特徴 | Topotecan is a water-soluble derivative of camptothecin. |
細胞アッセイ | 細胞株 | MCF-7 Luc and DU-145 Luc cells |
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濃度 | 0 μg/mL - 0.692 μg/mL | |
反応時間 | 96 hours | |
実験の流れ | Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×104 cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO2. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent imager. |
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動物実験 | 動物モデル | Mice with MCF-7 Luc or DU-145 Luc cells |
投薬量 | 0.25 mg/mL | |
投与方法 | Administered via i.p. |
Data from [Data independently produced by PLoS Genet, 2014, 10(1), e1004107]
Data from [Data independently produced by , , BMC Cancer, 2015, 10.1186/s12885-015-1231-z]
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] | PubMed: 38155773 |
Deneddylation of ribosomal proteins promotes synergy between MLN4924 and chemotherapy to elicit complete therapeutic responses [ Cell Rep, 2023, 42(8):112925] | PubMed: 37552601 |
p53 controls choice between apoptotic and non-apoptotic death following DNA damage [ bioRxiv, 2023, 2023.01.17.524444] | PubMed: 36712034 |
FL118, acting as a 'molecular glue degrader', binds to dephosphorylates and degrades the oncoprotein DDX5 (p68) to control c-Myc, survivin and mutant Kras against colorectal and pancreatic cancer with high efficacy [ Clin Transl Med, 2022, 12(5):e881] | PubMed: 35604033 |
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182] | PubMed: 36248745 |
Secreted HSP90α-LRP1 Signaling Promotes Tumor Metastasis and Chemoresistance in Pancreatic Cancer [ Int J Mol Sci, 2022, 23(10)5532] | PubMed: 35628341 |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Terfenadine resensitizes doxorubicin activity in drug-resistant ovarian cancer cells via an inhibition of CaMKII/CREB1 mediated ABCB1 expression [ Front Oncol, 2022, 12:1068443] | PubMed: 36439493 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
Ricolinostat suppresses proliferation, promotes apoptosis, and enhances the antiproliferative activity of topoisomerase inhibitors in cervical cancer cells [ Drug Dev Res, 2022, 10.1002/ddr.21999] | PubMed: 36173896 |
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。
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