Genz-644282
Catalog No.
A3434
拓扑异构酶I的非喜树碱抑制剂
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Description:
IC50 Value: 1.2 nM [1]
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].
Clinical trial: Dose-Escalation Study to Assess the Safety and Tolerability of Genz-644282 in Patients With Solid Tumors. Phase 1
Storage | Store at -20°C |
M.Wt | 407.42 |
Cas No. | 529488-28-6 |
Formula | C22H21N3O5 |
Synonyms | Genz644282;Genz 644282 |
Solubility | Soluble in DMSO |
Chemical Name | 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 |
SDF | Download SDF |
Canonical SMILES | O=C1N(C([H])([H])C([H])([H])N([H])C([H])([H])[H])C(C(C(N=C2[H])=C3[H])=C([H])C4=C3OC([H])([H])O4)=C2C(C1=C5[H])=C([H])C(OC([H])([H])[H])=C5OC([H])([H])[H] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |