| Identification | Back Directory | [Name]
Debio 0932 ,CUDC-305 | [CAS]
1061318-81-7 | [Synonyms]
CS-1423
CUDC-305
bio 0932
Debio 0932
Debio 0932 ,CUDC-305
CUDC-305 (DEBIO-0932 )
1H-Imidazo[4,5-c]pyridine-1-ethanamine, 4-amino-2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]thio]-N-(2,2-dimethylpropyl)- | [Molecular Formula]
C22H30N6O2S | [MOL File]
1061318-81-7.mol | [Molecular Weight]
442.58 |
| Chemical Properties | Back Directory | [Boiling point ]
654.8±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:33.0(Max Conc. mg/mL);74.56(Max Conc. mM) | [form ]
A crystalline solid | [pka]
10.02±0.19(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively[1]. | [in vivo]
Debio 0932 (CUDC-305, 30 mg/kg, p.o.) exhibits favorable pharmacokinetic profiles in tumor-bearing nude mice. Debio 0932 (160 mg/kg, p.o.) causes degradation of HSP90 client proteins, suppresses tumor growth, and also prolongs survival in various animal models of U87MG glioblastoma. Debio 0932 (40, 80, or 160 mg/kg, p.o.) also dose-dependently inhibits tumor growth in the U87MG s.c. tumor model by every-other-day (q2d) dosing[1]. Debio 0932 (80 mg/kg, p.o.) significantly alleviates psoriasis by day 11 and decreases epidermal thickness in psoriasis xenograft transplantation model[2]. Debio 0932 (CUDC-305) is able to cross the blood-brain barrier. Debio 0932 (80, 120, and 160 mg/kg, p.o.) shows dose-dependent inhibition of tumor growth in the H1975 subcutaneous tumor model. Debio 0932 (160 mg/kg, p.o.) also promotes antitumor activity in the erlotinib-resistant H1975 subcutaneous tumor model[3]. | [IC 50]
HSP90α: 100 nM (IC50); HSP90β: 103 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Bao R, et al. CUDC-305, a novel synthetic HSP90 inhibitor with unique pharmacologic properties for cancer therapy. Clin Cancer Res. 2009 Jun 15;15(12):4046-57. DOI:10.1158/1078-0432.CCR-09-0152
[2] Stenderup K, et al. Debio 0932, a new oral Hsp90 inhibitor, alleviates psoriasis in a xenograft transplantation model. Acta Derm Venereol. 2014 Nov;94(6):672-6. DOI:10.2340/00015555-1838
[3] Bao R, et al. Targeting heat shock protein 90 with CUDC-305 overcomes erlotinib resistance in non-small cell lung cancer. Mol Cancer Ther. 2009 Dec;8(12):3296-306. DOI:10.1158/1535-7163.MCT-09-0538 |
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