Topotecan Hydrochloride - CAS 119413-54-6
Catalog number: B0084-055461
Category: Inhibitor
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Molecular Formula:
C23H24ClN3O5
Molecular Weight:
457.91
COA:
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Targets:
Topoisomerase
Description:
Topocecan is a semisynthetic derivative of camptothecin with antineoplastic activity. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Camptothecin is a cytotoxic quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-055461 1 g $195 In stock
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Purity:
>98%
Synonyms:
SK&F 104864-A; SKF 104864A; SKFS 104864A; NSC 609669; Nogitecan hydrochloride
MSDS:
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InChIKey:
DGHHQBMTXTWTJV-BQAIUKQQSA-N
InChI:
InChI=1S/C23H23N3O5.ClH/c1-4-23(30)16-8-18-20-12(9-26(18)21(28)15(16)11-31-22(23)29)7-13-14(10-25(2)3)19(27)6-5-17(13)24-20;/h5-8,27,30H,4,9-11H2,1-3H3;1H/t23-;/m0./s1
Canonical SMILES:
CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=C(C5=C4)CN(C)C)O)O.Cl
1.Topotecan Delivery to the Optic Nerve after Ophthalmic Artery Chemosurgery.
Taich P1,2, Requejo F3, Asprea M4, Sgroi M5, Gobin P6, Abramson DH6, Chantada G7, Schaiquevich P1,2. PLoS One. 2016 Mar 9;11(3):e0151343. doi: 10.1371/journal.pone.0151343. eCollection 2016.
Extraocular retinoblastoma is a major challenge worldwide, especially in developing countries. Current treatment involves the administration of systemic chemotherapy combined with radiation, but there is a clear need for improvement of chemotherapy bioavailability in the optic nerve. Our aim was to study the ophthalmic artery chemosurgery (OAC) local route for drug delivery assessing ocular and optic nerve exposure to chemotherapy and to compare it to exposure after intravenous infusion (IV) of the same dose in an animal model. Topotecan was used as a prototype drug that is active in retinoblastoma and based on the extensive knowledge of its pharmacokinetics in preclinical and clinical settings. Five Landrace pigs received 4mg of topotecan via OAC as performed in retinoblastoma patients. At the end of the infusion, the eyes were enucleated, the optic nerve and retina were dissected, and the vitreous and plasma were separated. After recovery and a wash-out period, the animals received a 30-min IV infusion of topotecan (4 mg).
2.Treatment for small cell lung cancer, where are we now?-a review.
Alvarado-Luna G1, Morales-Espinosa D1. Transl Lung Cancer Res. 2016 Feb;5(1):26-38. doi: 10.3978/j.issn.2218-6751.2016.01.13.
Small cell lung cancer (SCLC) represents between 13% and 15% of all diagnosed lung cancers worldwide. It is an aggressive neoplasia, with a 5-year mortality of 90% or more. It has historically been classified as limited disease (LD) and extensive disease (ED) in most study protocols. The cornerstone of treatment for any stage of SCLC is etoposide-platinum based chemotherapy; in limited stage (LS), concomitant radiotherapy to thorax and mediastinum. Prophylactic radiotherapy to the central nervous system (CNS) [prophylactic cerebral irradiation (PCI)] has diminished the incidence of brain metastasis as the site for relapse in LD and ED patients, therefore it should be offered to patients with complete response to induction first-line treatment. Regarding second-line treatment, results are more modest and topotecan is accepted as treatment for this scenario offering a modest benefit.
3.Targeting Survivin Enhances Chemosensitivity in Retinoblastoma Cells and Orthotopic Tumors.
Ferrario A1, Luna M1, Rucker N1, Wong S1, Lederman A1, Kim J1,2, Gomer C1,3. PLoS One. 2016 Apr 6;11(4):e0153011. doi: 10.1371/journal.pone.0153011. eCollection 2016.
Treatments for retinoblastoma (Rb) vary depending on the size and location of the intraocular lesions and include chemotherapy and radiation therapy. We examined whether agents used to treat Rb induce a pro-survival phenotype associated with increased expression of survivin, a member of the inhibitor of apoptosis family of proteins. We document that exposure to carboplatin, topotecan or radiation resulted in elevated expression of survivin in two human Rb cell lines but not in normal retinal pigmented epithelial (RPE) cells. Cellular levels of survivin were attenuated in Rb cells exposed to an imidazolium-based survivin suppressant, Sepantronium bromide (YM155). Protein expression patterns of survivin in RPE cells were not altered following treatment protocols involving exposure to YM155. Including YM155 with chemotherapy or radiation increased levels of apoptosis in Rb cells but not in RPE cells. Intraocular luciferase expressing Rb tumors were generated from the Rb cell lines and used to evaluate the effects of carboplatin and YM155 on in-vivo survivin expression and tumor growth.
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CAS 119413-54-6 Topotecan Hydrochloride

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