ChemicalBook--->CAS DataBase List--->529488-28-6

529488-28-6

529488-28-6 Structure

529488-28-6 Structure
IdentificationBack 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
Questions And AnswerBack Directory
[Uses]

GENZ-644282 is used in the synthesis of ARC-111 analogs in the improvement of the antitumor activity of the parent compound.
Chemical PropertiesBack 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 InformationBack 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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