Genz644282
Uses- Product Name
- Genz644282
- CAS No.
- 529488-28-6
- Chemical Name
- Genz644282
- Synonyms
- CS-1079;GNZ-644282;Genz644282;GNZ-644282cas;GENZ644282; GENZ 644282;GENZ-644282;GENZ644282;GENZ 644282;Genz 644282,Inhibitor,inhibit,Genz-644282,Topoisomerase;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]-
- CBNumber
- CB12627899
- Molecular Formula
- C22H21N3O5
- Formula Weight
- 407.42
- MOL File
- 529488-28-6.mol
Genz644282 Property
- 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
N-Bromosuccinimide Price
- Product number
- 24193
- Product name
- Genz-644282
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $40
- Updated
- 2024/03/01
- Product number
- 24193
- Product name
- Genz-644282
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $186
- Updated
- 2024/03/01
- Product number
- 24193
- Product name
- Genz-644282
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $351
- Updated
- 2024/03/01
- Product number
- 24193
- Product name
- Genz-644282
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $728
- Updated
- 2024/03/01
- Product number
- G367760
- Product name
- GENZ-644282
- Packaging
- 50mg
- Price
- $1215
- Updated
- 2021/12/16
Genz644282 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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View Lastest Price from Genz644282 manufacturers
- Product
- Genz644282 529488-28-6
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 200kg
- Release date
- 2020-01-10