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Debio 0932

Catalog No. T15088 CAS 1061318-81-7

Synonyms: CUDC-305

Debio 0932 is an orally active inhibitor of HSP90 (IC50s: 100 and 103 nM for HSP90α and HSP90β, respectively).

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Debio 0932, CAS 1061318-81-7

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 64.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Debio 0932 is an orally active inhibitor of HSP90 (IC50s: 100 and 103 nM for HSP90α and HSP90β, respectively).
Targets&IC50	HSP90 β:103 nM, HSP90 α:100 nM
In vitro	Debio 0932 also displays inhibitory activities against the proliferation of 40 cancer cell lines (containing 34 solid and 6 hematologic tumor-derived lines) (IC50 ranging from 40 to 900 nM) (mean IC50, 220 nM) [1]. Debio 0932 binds to the tumor HSP90 complex( a mean IC50: 48.8 nM). Debio 0932 (1 μM) promotes degradation of multiple HSP90 client proteins in cancer cell lines. Debio 0932 potently binds to cancer-derived HSP90 complex (IC50: 61.2 nM in H1975 cells and 74.2 nM in H1993 cells, respectively). Debio 0932 (CUDC-305, 1 μM) durably induces oncoprotein degradation in NSCLC cell lines with mutations that can confer resistance to erlotinib [3].
In vivo	Debio 0932 is capable of penetrating the blood-brain barrier and demonstrates favorable pharmacokinetic properties in tumor-bearing nude mice at a dosage of 30 mg/kg orally. At 80 mg/kg orally, it significantly reduces symptoms of psoriasis by day 11 and lessens epidermal thickness in a psoriasis xenograft transplantation model [2]. Furthermore, a dose of 160 mg/kg orally leads to the degradation of HSP90 client proteins, inhibiting tumor growth and extending survival in various U87MG glioblastoma animal models. This dosage also enhances antitumor effects in an erlotinib-resistant H1975 subcutaneous tumor model. Dose-dependent suppression of tumor growth in the U87MG subcutaneous (s.c.) tumor model is observed with oral doses of 40, 80, or 160 mg/kg administered every other day (q2d) [1]. Additionally, oral doses of 80, 120, and 160 mg/kg exhibit a dose-dependent reduction of tumor growth in the H1975 subcutaneous tumor model [3].

Synonyms	CUDC-305
Molecular Weight	442.58
Formula	C22H30N6O2S
CAS No.	1061318-81-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33 mg/mL (74.56 mM)

References and Literature

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. 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. 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.

Citations

1. Lu X Y, Shi X J, Hu A, et al. Feeding induces cholesterol biosynthesis via the mTORC1–USP20–HMGCR axis. Nature. 2020, 588(7838): 479-484.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Debio 0932 1061318-81-7 Cytoskeletal Signaling Metabolism HSP CUDC 305 CUDC-305 CUDC305 inhibitor inhibit

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