- Genz644282
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- $1.00 / 1g
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2020-01-13
- CAS:529488-28-6
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 200kg
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| | Genz644282 Basic information | | Uses |
| Product Name: | Genz644282 | | Synonyms: | 2,3-Dimethoxy-12-[2-(methylamino)ethyl]benzo[c][1,3]benzodioxolo[5,6-h][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;GENZ-644282;GENZ644282;GENZ 644282;Genz644282;GNZ-644282;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;8,9-dimethoxy-2,3-methylenedioxy-5-[2-(N-methylamino)ethyl]-5H-dibenzo[c,h]1,6-naphthyridin-6-one;GENZ644282; GENZ 644282 | | CAS: | 529488-28-6 | | MF: | C22H21N3O5 | | MW: | 407.42 | | EINECS: | | | Product Categories: | | | Mol File: | 529488-28-6.mol |  |
| | Genz644282 Chemical Properties |
| 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 |
| | Genz644282 Usage And Synthesis |
| Uses | GENZ-644282 is used in the synthesis of ARC-111 analogs in the improvement of the antitumor activity of the parent compound. | | Uses | GENZ-644282 is used in the synthesis of ARC-111 analogs in the improvement of the antitumor activity of the parent compound. | | 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] |
| | Genz644282 Preparation Products And Raw materials |
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