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    Debio 0932 (CUDC-305)
    Debio 0932 (CUDC-305)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V3430
    CAS #: 1061318-81-7 Purity ≥98%

    Description: Debio 0932 (also known as CUDC-305) is a novel, potent and orally bioactive HSP90 (heat shock protein 90) inhibitor with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively. CUDC-305 binds strongly to HSP90 extracted from erlotinib-resistant NSCLC cells (IC50 70 nmol/L). This result correlates well with the potent antiproliferative activity in erlotinib-resistant NSCLC cell lines (IC50 120-700 nmol/L) reported previously. Furthermore, it exhibits durable inhibition of multiple oncoproteins and induction of apoptosis in erlotinib-resistant NSCLC cells. CUDC-305 potently inhibits tumor growth in subcutaneous xenograft models of H1975 and A549, which harbor EGFR T790M mutation or K-ras mutations conferring acquired and primary erlotinib resistance, respectively. In addition, CUDC-305 significantly prolongs animal survival in orthotopic lung tumor models of H1975 and A549, which may be partially attributed to its preferential exposure in lung tissue. Furthermore, CUDC-305 is able to extend animal survival in a brain metastatic model of H1975, further confirming its ability to cross the blood-brain barrier. Correlating with its effects in various tumor models, CUDC-305 induces degradation of receptor tyrosine kinases and downstream signaling molecules of the PI3K/AKT and RAF/MEK/ERK pathways simultaneously, with concurrent induction of apoptosis in vivo. In a combination study, CUDC-305 enhanced the antitumor activity of a standard-of-care agent in the H1975 tumor model. These results suggest that CUDC-305 holds promise for the treatment of NSCLC with primary or acquired resistance to EGFR inhibitor therapy.

    References:  2009 Dec;8(12):3296-306;  2014 Nov;94(6):672-6. 

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    Debio 0932 (CUDC-305)

    Name: Debio-0932 (CUDC305)
    CAS#: 1061318-81-7
    Chemical Formula: C22H30N6O2S
    Exact Mass: 442.21509
    Molecular Weight: 442.5776
    Elemental Analysis: C, 59.70; H, 6.83; N, 18.99; O, 7.23; S, 7.25
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: CUDC305; CUDC-305; CUDC 305; Debio0932; Debio-0932; Debio 0932.
    Chemical Name: 2-((6-(dimethylamino)benzo[d][1,3]dioxol-5-yl)thio)-1-(2-(neopentylamino)ethyl)-1H-imidazo[4,5-c]pyridin-4-amine
    InChi Code: InChI=1S/C18H18Cl2N6OS/c1-22-18-23-5-4-14(26-18)17-24-9-15(28-17)16(27)25-12(8-21)6-10-2-3-11(19)7-13(10)20/h2-5,7,9,12H,6,8,21H2,1H3,(H,25,27)(H,22,23,26)/t12-/m0/s1
    SMILES Code: O=C(C1=CN=C(C2=NC(NC)=NC=C2)S1)N[[email protected]@H](CC3=CC=C(Cl)C=C3Cl)CN

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    Debio 0932 (CUDC-305)

    CUDC-305 binding affinity to HSP90 complex from NSCLC cell extracts.

    Debio 0932 (CUDC-305)

    A, pharmacodynamic study in K-ras–mutated A549 subcutaneous tumors.   2009 Dec;8(12):3296-306

     Debio 0932 (CUDC-305)

    A, schematic representation of the experimental design. Debio 0932 (CUDC-305)

    A, efficacy study in the H1975 orthotopic lung tumor model compared with erlotinib (n = 10).  2009 Dec;8(12):3296-306

     Debio 0932 (CUDC-305)

    A, CUDC-305 concentration-over-time curves in the lung, compared with other tissues following a single oral dose of CUDC-305 at 30 mg/kg.  2009 Dec;8(12):3296-306


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