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Formula | C23H23N3O5.HCl |
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Molecular Weight | 457.91 | CAS No. | 119413-54-6 | |
Solubility (25°C)* | In vitro | DMSO | 92 mg/mL (200.91 mM) | |
Water | 92 mg/mL (200.91 mM) | |||
Ethanol | Insoluble | |||
* <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 | 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] |
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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] |
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Features | Topotecan is a water-soluble derivative of camptothecin. |
Cell Assay: |
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Animal Study: |
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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]
The splicing factor CCAR1 regulates the Fanconi anemia/BRCA pathway [ Mol Cell, 2024, 84(14):2618-2633.e10] | PubMed: 39025073 |
Synergistic antitumor effect of liposomal-based formulations of olaparib and topotecan in primary epithelial ovarian cancer cells [ Cancer Cell Int, 2024, 24(1):285] | PubMed: 39135053 |
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] | PubMed: 38155773 |
Topotecan and Ginkgolic Acid Inhibit the Expression and Transport Activity of Human Organic Anion Transporter 3 by Suppressing SUMOylation of the Transporter [ Pharmaceutics, 2024, 16(5)638] | PubMed: 38794300 |
AAV-mediated genome editing is influenced by the formation of R-loops [ bioRxiv, 2024, 2024.05.07.592855] | PubMed: 38766176 |
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 |
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