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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Topoisomerase-Genz-644282
Genz-644282

Chemical Structure : Genz-644282

CAS No.: 529488-28-6

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Genz-644282 (Genz 644282)

货号: PC-22288Not For Human Use, Lab Use Only.

Genz-644282 is a potent, non-camptothecin topoisomerase I (Top1) inhibitor, shows potent activities against a panel of human tumor cell lines with IC50 of 1.8 nM-1.8 uM.

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5 mg ￥880 In stock
10 mg ￥1380 In stock
50 mg ￥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Genz-644282 is a potent, non-camptothecin topoisomerase I (Top1) inhibitor, shows potent activities against a panel of human tumor cell lines with IC50 of 1.8 nM-1.8 uM.
Genz-644282 suppresses the PPTP cell lines mean IC50 value of 1.2 nM.
Genz-644282 (0.1 μM) induces γH2AX foci in human colon cancer HCT116 cells and breast cancer MCF7 cells.
Genz-644282 is not a substrate for the multidrug resistance gene 1 (MDR1) and breast cancer resistance protein (BCRP) efflux pumps, contrary to the camptothecins.
Administration of Genz-644282 (1.7 mg/kg) produced a TGD of 23 days in mice bearing 786-O tumors compared with a TGD of 16 days after administration of irinotecan (60 mg/kg), with maximum T/Cs of 8.7% and 20.7%, respectively.

物理化学性质&存储条件

分子量 407.43
分子式 C22H21N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Kurtzberg LS, et al. Clin Cancer Res. 2011 May 1;17(9):2777-87.

2. Sooryakumar D, et al. Mol Cancer Ther. 2011 Aug;10(8):1490-9.

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