| Name | Debio 0932 |
| Description | Debio 0932 (CUDC-305) is a heat shock protein 90 (Hsp90) inhibitor that targets the n-terminal atp-binding pocket to promote apoptosis, and has the advantage of being orally available and able to cross the blood-brain barrier (BBB) for the treatment of cancers such as non-small-cell lung cancer (NSCLC) and neuroblastoma. |
| In vitro | Debio 0932 exhibits dose- and time-dependent proliferation inhibition in MCF-7 and MDA-MB-231 cells, with IC50 values of 6.19 µM and 10.66 µM at 48 hours, respectively. It promotes apoptosis by upregulating Bax/Bcl-2, activating Caspase-9, and inhibiting HUVEC migration [1]. In NSCLC, the IC50 values against A549, H1299, and H1975 cells are 3.26±2.82 µM, 20.33±5.39 µM, and 3.16±1.04 µM, respectively. It induces cell cycle arrest and apoptosis, and targets Hsp90 with an IC50 value of 70 nmol/L, leading to the degradation of mutant EGFR and K-RAS, thus reversing erlotinib resistance [2,3]. |
| In vivo | In a psoriasis xenograft model, treatment with Debio 0932 (80 mg/kg, orally daily) for 3 weeks resulted in a significant clinical improvement by day 11, with a marked reduction in epidermal thickness [4]. In the U87MG glioblastoma mouse model, treatment with Debio 0932 (160 mg/kg, every other day) induced tumor regression. In an acute myeloid leukemia (AML) mouse model, after 3 weeks of treatment with Debio 0932 (160 mg/kg, every other day), complete tumor regression was observed, with good drug safety [5]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.52 mM), Sonication is recommended.
DMSO : 60 mg/mL (135.57 mM), Sonication is recommended.
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| Keywords | HSP90β | HSP90α | Debio 0932 | CUDC 305 |
| Inhibitors Related | Ethoxyquin | Adezmapimod | Tamoxifen | Palmitic acid sodium | Mequinol | 7-Aminocephalosporanic acid | Benzbromarone | Elesclomol | Rifabutin | Palmitic acid | Tamoxifen Citrate | Isoxazole |
United States
