17-DMAGbindstoHsp90andaltersitsfunction.Awatersolublecell-permeableanalogofGeldanamycin(G-1047)and17-AAG(A-1256),17-DMAGbindstotheAPTasesiteofhumanHsp90awithhighaffinity,hascytotoxicactivityagainstmanycancercelllines,andactsasangiogenesisinhibitor.Treatmentwith17-DMAGsignificantlyreducedthehemorrhage-inducedincreasesiniNOSprotein,jejunalalteration,andIL-10concentrations,but17-DMAGdidnotaffectthehemorrhage-inducedincreasesinp53andIL-6concentration.17-DMAGdiminisheshemorrhage-inducedsmallintestineinjurybyelevatingBcl-2proteinandinhibitingiNOSpathway,TNF-alphaincrease,andcaspase-3activation.HSP90inhibits,17-(dimethylaminoethylamino)-17-demethoxygeldanamycin(DMAG)toincreasetherADIosensitivityoftumorcellsinvitro.HSP90inhibitor,17-DMAG,enhancesradiosensitivityofhumancancercells.
AdditionalInformation
| Synonyms | NSC707545 |
|---|---|
| Product# | A-1298 |
| CAS# | 467214-20-6 |
| ChemicalName | 17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin |
| Formula | C32H48N4O8 |
| MW | 616.8 |
| Appearance | PurplePowder |
| Purity | 98%byTLC |
| Solubility | SolubleinDMSO,Methanol,Ethanol |
| BoilingPoint | 810.5±65.0°Cat760mmHg |
| Preparation | Clearpurplesolutionat10mg17DMAGin1mlofMethanol,or25mg17DMAGin1mlDMSO |
| StorageTemp | -20°C |
| TherapeuticArea | OncologicalDisorders |
| Use | 17-DMAGisusedtoinhibitcancergrowthandtopromoteapoptosisinmultiplecelllines |
| MDLNumber | MFCD08457919 |
|---|---|
| ChemACX | X1578552-3 |
| InChI | InChI=1S/C32H48N4O8/c1-18-14-22-27(34-12-13-36(5)6)24(37)17-23(29(22)39)35-31(40)19(2)10-9-11-25(42-7)30(44-32(33)41)21(4)16-20(3)28(38)26(15-18)43-8/h9-11,16-18,20,25-26,28,30,34,38H,12-15H2,1-8H3,(H2,33,41)(H,35,40)/b11-9-,19-10+,21-16+/t18-,20+,25+,26+,28-,30+/m1/s1 |
| SMILES | C[C@H]1C[C@@H]([C@@H]([C@H](/C=C(/[C@@H]([C@H](/C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)/C)OC)OC(=O)N)C)C)O)OC |
