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    Danusertib (PHA739358)
    Danusertib (PHA739358)

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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 #: V0348
    CAS #: 827318-97-8Purity ≥98%

    Description: Danusertib (formerly PHA-739358), a pyrrolo-pyrazole compound, is a potent Aurora kinase inhibitor of Aurora A/B/C with potential antitumor activity. It inhibits Aurora A/B/C with IC50s of 13 nM, 79 nM and 61 nM in cell-free assays, odestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib is a potent small-molecule inhibitor of aurora kinases family members with a dominant inhibition for aurora B kinase (ABK). It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. It has the potential for treating chronic myelogenous leukemia (CML), acute lymphoblastic leukemia (ALL), thyroid prostate and breast carcinoma. 

    References: Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.

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    Molecular Weight (MW)474.55
    CAS No.827318-97-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 95 mg/mL (200.2 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL (slightly soluble or insoluble)
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL
    Chemical Name/Synonyms

    Synonym: Danusertib; PHA-739358; PHA 739358; PHA739358; 

    Chemical Name: (R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide


    InChi Code: InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1

    SMILES Code: O=C(NC1=NNC2=C1CN(C([[email protected]](OC)C3=CC=CC=C3)=O)C2)C4=CC=C(N5CCN(C)CC5)C=C4 

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    In VitroDanusertib inhibits the activities of other kinases such as FGFR1, Abl, Ret and Trka, with IC50 of 47 nM, 25 nM, 31 nM and 31 nM, respectively. In a cell assay, after treatment of wild-type and p53-deficient MEFs with Danusertib, the wild-type cells undergo an arrest in mitosis (4N) that is maintained for up to 48 h.
    In VivoAdministration of 25 mg/kg Danusertib (b.d. i.v.) to HL-60 xenograft rats results in 75% inhibition of tumor growth with complete regression in one animal. Danusertib significantly inhibits proliferation of K562 cells and virtually suppressed tumor growth during the 10-day treatment period.
    Animal modelFemale SCID mice
    Formulation & Dosage DMSO; 15 mg/kg; i.p.
    References[1] Gontarewicz A, et al. Blood, 2008, 111(8), 4355-4364.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Danusertib (PHA-739358)

    Danusertib (PHA-739358)

    Inhibition of cellular pathways by PHA-739358. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.

    Danusertib (PHA-739358)

    PHA-739358 treatment results in the inhibition of tumor growth in TRAMP mice as assessed by MRI evaluation. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.


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