| Identification | Back Directory | [Name]
Genz644282 | [CAS]
529488-28-6 | [Synonyms]
CS-1079
Genz644282
GNZ-644282
GENZ644282; GENZ 644282
GENZ-644282;GENZ644282;GENZ 644282
8,9-dimethoxy-2,3-methylenedioxy-5-[2-(N-methylamino)ethyl]-5H-dibenzo[c,h]1,6-naphthyridin-6-one
2,3-Dimethoxy-12-[2-(methylamino)ethyl]benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one
Benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one, 2,3-dimethoxy-12-[2-(methylamino)ethyl]-
2,3-dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5':4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one
2,3-Dimethoxy-12-[2-(methylamino)ethyl]benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one GENZ-644282 | [Molecular Formula]
C22H21N3O5 | [MDL Number]
MFCD25976816 | [MOL File]
529488-28-6.mol | [Molecular Weight]
407.42 |
| Chemical Properties | Back Directory | [Melting point ]
254-257℃ (Decomposition) | [Boiling point ]
665.5±55.0 °C(Predicted) | [density ]
1.344±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
Chloroform (Slightly) | [form ]
Solid | [pka]
9.59±0.10(Predicted) | [color ]
Off-White to Pale Yellow |
| Hazard Information | Back Directory | [Biological Activity]
genz-644282 [8,9-dimethoxy-5-(2-n-methylaminoethyl)-2,3-methylenedioxy-5h-dibenzo[c,h][1,6]naphthyridin-6-one] has emerged as a promising candidate of non-camptothecin topoisomerase i inhibitor for antitumor agents. | [in vitro]
genz-644282 demonstrated potent cytotoxic activity with a median ic(50) of 1.2 nm (range 0.2-21.9 nm) [1]. limited cross-resistance to genz-644282 was also found in the top1 knockdown colon cancer (hct116) and breast cancer (mcf7) cell lines and in human adenocarcinoma cells (kb31/kbv1) that overexpress (p-glycoprotein, abcb1), a member of the atp-binding cassette family of cell surface transport proteins known to confer mdr [3]. | [in vivo]
genz-644282 at its mtd (4 mg/kg) induced maintained complete responses (mcr) in 6/6 evaluable solid tumor models. at 2 mg/kg genz-644282 induced cr or mcr in 3/3 tumor models relatively insensitive to topotecan, but there were no objective responses at 1 mg/kg [1]. genz-644282 was tolerated at doses up to 4 mg/kg when administered intravenously on alternate days, and the compound was active at doses from 1 to 4 mg/kg. the efficacy of genz-644282 was compared with irinotecan in 4 human colon carcinoma xenograft models. in the human hct-116 colon cancer xenograft, tgd values were 14 days for irinotecan (60 mg/kg) and 34 days for genz-644282 (2.7 mg/kg), giving maximum test to control ratios (t/cs) of 23.7% and 16.8%, respectively [2]. | [IC 50]
1.2 nm [1] | [storage]
4°C, protect from light |
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