An inhibitor of topoisomerase I that inhibits topoisomerase I-mediated DNA cleavage 10-fold more potently than topotecan; inhibits the growth of and is cytotoxic to human and mouse bone marrow cells in vitro (IC50s = 0.4 and 2.3 nM

Genz-644282 – 5 mg

Brand:
Cayman
CAS:
529488-28-6
Storage:
-20
UN-No:
Non-Hazardous - /

Genz-644282 is a topoisomerase I (TOP-I) inhibitor that inhibits TOP-I-mediated DNA cleavage 10-fold more potently than the TOP-I inhibitor topotecan (Item No. 14129).{41650} It inhibits the growth of and is cytotoxic to human and mouse bone marrow cells in a colony-forming unit assay (IC50s = 0.4 and 2.3 nM, respectively; IC90s = 1.2 and 8.4 nM, respectively).{41651} It also inhibits the growth of and is cytotoxic to human tumor cell lines (IC50s = 0.15-2 nM; IC90s = 0.7-8.3 nM). Genz-644282 inhibits tumor growth in mouse xenograft models when administered at doses ranging from 1.36 to 2.7 mg/kg.  

 

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SKU: 24193 - 5 mg Category:

Description

An inhibitor of topoisomerase I that inhibits topoisomerase I-mediated DNA cleavage 10-fold more potently than topotecan; inhibits the growth of and is cytotoxic to human and mouse bone marrow cells in vitro (IC50s = 0.4 and 2.3 nM, respectively; IC90s = 1.2 and 8.4 nM, respectively); inhibits the growth of and is cytotoxic to human tumor cell lines in vitro (IC50s = 0.15-2 nM; IC90s = 0.7-8.3 nM); inhibits tumor growth in mouse xenograft models (1.36-2.7 mg/kg)

Formal name: 2,3-dimethoxy-12-[2-(methylamino)ethyl]-benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one

Synonyms: 

Molecular weight: 407.4

CAS: 529488-28-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Topoisomerases||Research Area|Cancer|Cell Death||Research Area|Cancer|DNA Damage and Repair|Topoisomerase

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