Topotecan

Catalog No.S9321 Batch:S932104

Technical Data

Formula	C₂₃H₂₃N₃O₅
Molecular Weight	421.45	CAS No.	123948-87-8
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (199.31 mM)
		Water	Insoluble
		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.)

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Biological Activity

Description

Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

Targets

Topo I ^[1]

In vitro

Topotecan exhibits inhibition of outgrowth of the highly invasive and migratory leader cells (LC) population, however, topotecan enrichs the LC subset 20% above the untreated control level.^[2]

In vivo

Topotecan (TPT), at least in part by inhibiting expression of Fli-1, significantly ameliorates lupus nephritis in NZBWF1 mice as effectively or better than cyclophosphamide (CYC).^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines LC-T2A-GFP lines Concentrations 1 μM Incubation Time 72 h Method LC-T2A-GFP lines are seeded at 1200 cells per well of a 384-well plate, adhered overnight, and treated with chemotherapeutics olaparib, rucaparib, paclitaxel, topotecan, carboplatin, cyclophosphamide, cisplatin, and doxorubicin at empirically determined clinically relevant doses (1 μM). Cells are maintained at 37 ℃ with 5% CO₂ in treatment for 72 h. Four focal areas per replicate well were imaged using 4X magnification on a bright field.
Animal Study:^{^[3]}	Animal Models NZBWF1 female mice Dosages 0.03 mg/kg, 0.1 mg/kg, 0.3mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
LC-T2A-GFP lines
Concentrations
1 μM
Incubation Time
72 h
Method
LC-T2A-GFP lines are seeded at 1200 cells per well of a 384-well plate, adhered overnight, and treated with chemotherapeutics olaparib, rucaparib, paclitaxel, topotecan, carboplatin, cyclophosphamide, cisplatin, and doxorubicin at empirically determined clinically relevant doses (1 μM). Cells are maintained at 37 ℃ with 5% CO₂ in treatment for 72 h. Four focal areas per replicate well were imaged using 4X magnification on a bright field.

Animal Study:^{^[3]}

Animal Models
NZBWF1 female mice
Dosages
0.03 mg/kg, 0.1 mg/kg, 0.3mg/kg
Administration
i.p.

References

Selleck's Topotecan has been cited by 25 publications

Identification and targeting of protein tyrosine kinase 7 (PTK7) as an immunotherapy candidate for neuroblastoma [ Cell Rep Med, 2023, 4(6):101091]	PubMed: 37343516
Immune suppressive signaling regulated by latent transforming growth factor beta binding protein 1 promotes metastasis in cervical cancer [ Braz J Med Biol Res, 2023, 55:e12206]	PubMed: 36629522
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
Secreted HSP90α-LRP1 Signaling Promotes Tumor Metastasis and Chemoresistance in Pancreatic Cancer [ Int J Mol Sci, 2022, 23(10)5532]	PubMed: 35628341
Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan [ Molecules, 2022, 27(11)3374]	PubMed: 35684313
Immunogenicity of small-cell lung cancer associates with STING pathway activation and is enhanced by ATR and TOP1 inhibition [ Cancer Med, 2022, 10.1002/cam4.5109]	PubMed: 35957613
SMARCA4/2 loss inhibits chemotherapy-induced apoptosis by restricting IP3R3-mediated Ca2+ flux to mitochondria [ Nat Commun, 2021, 12(1):5404]	PubMed: 34518526
Camptothecin and topotecan, inhibitors of transcription factor Fli-1 and topoisomerase, markedly ameliorate lupus nephritis in NZBWF1 mice and reduce the production of inflammatory mediators in human renal cells [ Arthritis Rheumatol, 2021, 10.1002/art.41685]	PubMed: 33559345
Chemoresistance is mediated by ovarian cancer leader cells in vitro [ J Exp Clin Cancer Res, 2021, 40(1):276]	PubMed: 34470672
FK228 potentiates topotecan activity against small cell lung cancer cells via induction of SLFN11 [ Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00817-y]	PubMed: 34893686

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SHIPPING AND STORAGE
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