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Topotecan hydrochloride

Cat. No. M2144
Topotecan hydrochloride Structure
Synonym:

Hycamtin, NSC 609669

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 47  USD47 In stock
50mg USD 127  USD127 In stock
100mg USD 185  USD185 In stock
200mg USD 275  USD275 In stock
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Quality Control & Documentation
Biological Activity

Topotecan hydrochloride (trade name Hycamtin) is a potent antineoplastic agent. It is a water soluble analog of the alkaloid camptothecin that potently inhibits DNA topoisomerase I. Topotecan hydrochloride induces rapid apoptotic death in human B-lineage acute lymphoblastic leukemia (ALL) cells with IC50 values of 33 nM and 0.28 μM, respectively. Topotecan improves survival in three mouse models of poor prognosis ALL and downregulates B-Myb and MycN expression in neuroblastoma cells. Topotecan demonstrates a broad spectrum of antitumor activity against a variety of other tumors including ovarian cancer, cervical cancer, neuroblastoma, brainstem glioma, and Ewing’s sarcoma.

Product Citations
Customer Product Validations & Biological Datas
Source J Korean Med Sci (2016). Figure 5. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience (Shanghai, China).
Method CCK8 Assay and ABCG2 ATPase assay
Cell Lines RCSC cells
Concentrations 0~10 μM
Incubation Time 72 h
Results MiR-3163 plays important roles in multidrug resistance (Table 1, Fig. 5A). Results showed that when miR-3163 was overexpressed in RCSCs, the ATPase activity of ABCG2 was significantly downregulated compared to RCSCs with Scramble (Fig. 5B).
Chemical Information
Molecular Weight 457.91
Formula C23H23N3O5.HCl
CAS Number 119413-54-6
Solubility (25°C) DMSO 35 mg/mL
Water 33 mg/mL
Storage 2-8°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sottile F, et al. Oncotarget. A chemical screen identifies the chemotherapeutic drug topotecan as a specific inhibitor of the B-MYB/MYCN axis in neuroblastoma.

[2] Schellens JH, et al. Br J Cancer. Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor.

[3] Uckun FM, et al. Blood. In vitro and in vivo activity of topotecan against human B-lineage acute lymphoblastic leukemia cells.

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Keywords: Topotecan hydrochloride, Hycamtin, NSC 609669 supplier, Topoisomerase, inhibitors, activators


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