产品说明书

Genz-644282

Print
Chemical Structure| 529488-28-6 同义名 : -
CAS号 : 529488-28-6
货号 : A204687
分子式 : C22H21N3O5
纯度 : 99%+
分子量 : 407.419
MDL号 : MFCD25976816
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(7.36 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Genz-644282, identified as a potent topoisomerase I inhibitor, demonstrates significant efficacy across a spectrum of 29 human tumor cell lines with IC50 values ranging from 1.8 nM to 1.8 μM[1]. Genz-644282 exhibits substantial suppressive effects on the PPTP cell lines, with IC50 values between 0.2-21.9 nM and an average IC50 of 1.2 nM[2]. Furthermore, Genz-644282 is effective in stabilizing Top1-DNA covalent cleavage complexes, and at 0.1 μM, it induces γH2AX foci in both human colon cancer HCT116 cells and breast cancer MCF7 cells, demonstrating cytotoxicity in CPT-resistant human cancer cell lines[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.54mL

4.91mL

2.45mL
参考文献

[1]Kurtzberg LS, et al. Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment. Clin Cancer Res. 2011 May 1;17(9):2777-87.

[2]Houghton PJ, et al. Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Feb;58(2):200-9.

[3]Sooryakumar D, et al. Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282. Mol Cancer Ther. 2011 Aug;10(8):1490-9.