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Debio 0932 CAS: 1061318-81-7

Category: Inhibitors
Product Name: Debio 0932
Cat No: I000309
CAS No: 1061318-81-7
Molecular Formula: C22H30N6O2S
Molecular Weight: 442.58
SMILES: O=C(C1=CN=C(C2=NC(NC)=NC=C2)S1)N[C@@H](CC3=CC=C(Cl)C=C3Cl)CN
InChI: None
InChIKey: None
Solubility: DMSO: > 35 mg/mL
Target: target: HSP90 [1]
CAS 1061318-81-7,Debio 0932
  • Description

Debio 0932 ( CUDC-305 ) is a novel heat shock protein 90 (HSP90) inhibitor trong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L). [1]
in vitro: H1993 and H1975 NSCLC cells were incubated with 1 μmol/L CUDC-305 for 7 hours and then cultured in compound-free medium for an additional 0, 17, or 24 hours, respectively, before being analyzed by Western blot [1]
in vivo: CUDC-305 was delivered through oral gavage on an every-other-day (once every two days) dosing schedule at various doses up to 160 mg/kg-its maximum tolerated dose in nude mice. In survival studies in Balb/C nude mice, the highest dose was reduced to 120 mg/kg as a result of the compromised animal condition due to lung and brain tumor implantation surgeries. [1]

  • Spec

Appearance:white to off-white solid powder
Purity: > 98%

  • References

1:Acta Derm Venereol. 2014 Nov;94(6):672-6. doi: 10.2340/00015555-1838. Debio 0932, a new oral Hsp90 inhibitor, alleviates psoriasis in a xenograft transplantation model.Stenderup K,Rosada C,Gavillet B,Vuagniaux G,Dam TN, PMID: 24604074 DOI: 10.2340/00015555-1838
Abstract: Debio 0932 is a novel oral heat shock protein 90 (Hsp90) inhibitor developed for anti-cancer therapy. Surprising-ly, during the first clinical trial, one psoriasis patient experienced complete remission of his skin manifestation. However, a possible therapeutic utility of Hsp90 in psoriasis has not previously been reported. The objective of the present study was to explore the ability of Debio 0932 to alleviate psoriasis in a preclinical model. A psoriasis xenograft transplantation model was employed where skin from 5 psoriasis patients was transplanted onto immunodeficient mice (8 xenografts per donor). Debio 0932 was administered perorally daily for 3 weeks and resulted in significant clinical alleviation of psoriasis by day 11 and reduced epidermal thickness evaluated post-treatment. Alleviation of psoriasis in the psoriasis xenograft transplantation model, which may be due to Hsp90's involvement in signalling pathways that are up-regulated in psoriasis, substantiates a potential role of Debio 0932 in psoriasis treatment.


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