AZD5582 dihydrochloride
Axon 4139
- Parent CAS: 1258392-53-8
- Optical Purity: Optically pure
- Soluble in water and DMSO
- MF: C58H78N8O8.2HCl
- MW: 1088.21
Description
AZD5582 dihydrochloride is a cell permeable, novel class of dimeric SMAC mimetic designed to mimick the AVPI motif of SMAC. It is a potent and selective inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein with IC50 values of 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2, respectively. At nanomolar concentrations AZD5582 causes extensive degradation of cIAP-1 and cIAP-2, and induces apoptosis in MDA-MB-231 breast cancer cells. It causes substantial tumor regressions following two weekly doses of 3.0 mg/kg in MDA-MB-231 xenograft-bearing mice.
More Information
| Parent CAS No. | 1258392-53-8 |
|---|---|
| Chemical Name | (S,S,2S,2'S)-N,N'-((1S,1'S,2R,2'R)-2,2'-(Hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide) dihydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C(#CCO[C@@H]1CC2C=CC=CC=2[C@@H]1NC([C@H]1N(C([C@H](C2CCCCC2)NC(=O)[C@H](C)NC)=O)CCC1)=O)C#CCO[C@H]1[C@@H](NC([C@@H]2CCCN2C(=O)[C@H](C2CCCCC2)NC(=O)[C@H](C)NC)=O)C2C=CC=CC=2C1.Cl.Cl |&1:4,12,15,18,28,41,42,45,52,62,r| |
| MFCD | N.A. |
| InChi | N.A. |
| InChiKey | N.A. |
| CID | N.A. |
| Short Description | Apoptosis proteins (IAPs) inhibitor |
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