Debio 0932

SKU: orb1707393

Description

Debio 0932 (CUDC-305) is an orally bioavailable, brain-penetrant Hsp90 inhibitor that binds the N-terminal ATPase domain. It induces apoptosis and has demonstrated antitumor activity in preclinical in vitro and in vivo models for cancers including non-small cell lung cancer and neuroblastoma.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1061318-81-7
• MW: 442.58
• Purity: 98.98% (May vary between batches)
• Formula: C₂₂H₃₀N₆O₂S
• SMILES: N=1C=CC2=C(N=C(SC3=CC=4OCOC4C=C3N(C)C)N2CCNCC(C)(C)C)C1N
• Target: HSP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.52 mM);DMSO:60 mg/mL (135.57 mM)

Bioactivity

• Target IC50:
  H1299 cells:20.33±5.39 µM|A549 cells:3.26±2.82 µM|MDA-MB-231 cells:10.66 µm|MCF-7 cells:6.19 µM|HSP90 β:103 nM|HSP90 α:100 nM
• 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 . 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 .
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• 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 . 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].
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CUDC 305, CUDC305, CUDC-305, BEBT305, BEBT-305, HSP90α, HSP90β, Debio 0932, MC2-32, RGRN-305

Compound Identifiers

PubChem CID

44156921