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SML4288

GENZ-644282

≥98% (HPLC), powder, topoisomerase I inhibitor

Synonym(s):

2,3-Dimethoxy-12-[2-(methylamino)ethyl]benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one, Genz 644282

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About This Item

Empirical Formula (Hill Notation):
C22H21N3O5
CAS Number:
529488-28-6
Molecular Weight:
407.42
MDL number:
MFCD25976816
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Application

GENZ-644282 may be used to study its tumor cell colony-forming unit (CFU) activity in human tumor xenograft models. It is also used in molecular and cellular studies such as:

  • alkaline elution assay for the detection of Top1-DNA crosslinks
  • two-dimensional flow cytometry analysis for DNA and γH2AX
  • cytotoxicity assays

Biochem/physiol Actions

GENZ-644282 is a highly potent non-camptothecin topoisomerase I (Top1) inhibitor. Genz-644282 is approximately 20-fold more potent as an antitumor agent than irinotecan. Genz-644282 has been shown not to be a substrate for efflux transporters associated with multidrug resistance in cancer cells. GENZ-644282 functions by binding to the topoisomerase I-DNA cleavage complex, thereby stabilizing it. This action results in the formation of DNA breaks, which accumulate and ultimately trigger apoptotic pathways in cancer cells. Notably, the compound exhibits a longer persistence of the Top1 complexes compared to traditional inhibitors like camptothecin, which allows it to maintain its cytotoxic effects for extended periods.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302,H315

Hazard Classifications

Acute Tox. 4 Oral - Skin Irrit. 2

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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