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Genz 644282
Axon 2198
CAS:
529488-28-6
Purity:
99%
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C22H21N3O5
- MW: 407.42
Description
Topoisomerase I inhibitor (IC50 value 0.4 nM in human bone marrow CFU-GM assay). Cytotoxic agent, with activity toward 8 human tumor cell lines of varied histology and resistance mechanisms by colony formation, with enhanced potency compared to topotecan and SN-38. Contrary to the camptothecins, Genz-644282 is not a substrate for the multidrug resistance gene 1 (MDR1) and breast cancer resistance protein (BCRP) efflux pumps.
More Information
| Parent CAS No. | 529488-28-6 |
|---|---|
| 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 |
| SMILES | N1(CCNC)C2=C(C=NC3=CC4=C(C=C32)OCO4)C2=CC(OC)=C(OC)C=C2C1=O |
| MFCD | N.A. |
| InChi | InChI=1S/C22H21N3O5/c1-23-4-5-25-21-14-8-19-20(30-11-29-19)9-16(14)24-10-15(21)12-6-17(27-2)18(28-3)7-13(12)22(25)26/h6-10,23H,4-5,11H2,1-3H3 |
| InChiKey | BAORCAMWLWRZQG-UHFFFAOYSA-N |
| CID | 10294813 |
| Short Description | Topo 1 inhibitor |
References
- L.S. Kurtzberg et al. Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment. Clin. Cancer Res. 2011, 17, 2777-2787.
- P.J. Houghton et al. Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program. Pediatr. Blood Cancer. 2012, 58, 200-209.
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