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    Taselisib (GDC0032)
    Taselisib (GDC0032)

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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 #: V4531
    CAS #: 1282512-48-4Purity ≥98%

    Description: Taselisib (formerly also known as GDC-0032 or RG-7606), an imidazobenzoxazepin compound, is a novel and potent β-sparing small molecule inhibitor of PI3K with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. GDC-0032 has been progressed to clinical trials and is currently under phase I evaluation as a potential treatment for human malignancies. GDC-0032 has increased potency in HNSCC cell lines harboringPIK3CA-activating aberrations. Further, combined GDC-0032 and radiotherapy was more efficacious than either treatment alone inPIK3CA-altered HNSCCin vitro and in vivo. 

    References: J Med Chem. 2013 Jun 13;56(11):4597-610.Clin Cancer Res. 2016 Apr 15; 22(8): 2009–2019.Br J Cancer. 2016 Jul 26;115(3):303-11.


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    Taselisib

    Name: Taselisib (GDC0032)
    CAS#: 1282512-48-4
    Chemical Formula: C24H28N8O2
    Exact Mass: 460.23352
    Molecular Weight: 460.53
    Elemental Analysis: C, 62.59; H, 6.13; N, 24.33; O, 6.95
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: RG7604; RG7604; RG 7604; GDC0032, GDC0032, GDC 0032
    IUPAC/Chemical Name: 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide
    InChi Key: BEUQXVWXFDOSAQ-UHFFFAOYSA-N
    InChi Code: InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
    SMILES Code: CC(C)(N1N=CC(C2=CC=C3C4=NC(C5=NC(C)=NN5C(C)C)=CN4CCOC3=C2)=C1)C(N)=O


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    Taselisib


    GDC-0032 has greater antiproliferative activity in cells containing activating PIK3CA alterations, whereas PTEN mutation or loss is associated with resistance to this agent.  2016 Apr 15;22(8):2009-19.

    Taselisib


    GDC-0032 enhances the G2–M checkpoint following irradiation in an ATR-dependent manner.  2016 Apr 15;22(8):2009-19.

     Taselisib


    GDC-0032 enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activity.  2016 Apr 15;22(8):2009-19.

     Taselisib


    GDC-0032 decreases clonogenicity and impairs DNA damage in Cal-33 following irradiation.   2016 Apr 15;22(8):2009-19.

    Taselisib


    GDC-0032 is a more potent inhibitor of downstream AKT and mTOR signaling in head and neck cancer cell lines containing PIK3CA-activating alterations than in cell lines containing PTEN alterations.

     Taselisib


    GDC-0032 potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy in vivo. 2016 Apr 15;22(8):2009-19.


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