Pilaralisib(XL-147; SAR245408)|Supplied by DC Chemicals

  • Published on
    11-Dec-2015

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  • Datasheet of XL-147

    Description:

    XL147(SAR245408; pilaralisib) is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50

    values of 39 nM/383 nM/36 nM/23 nM for PI3K///, respectively; less potent to PI3K.

    in vitro: XL147 binds in an ATP-competitive and reversible manner, yet is highly selective against a panel of >130 human

    protein kinases. In cellular assays, XL147 antagonizes the production of the second messenger

    phosphatidylinositol-3,4,5-trisphosphate (PIP3) resulting in inhibition of phosphorylation of several downstream effectors of

    PI3K including Akt, ribosomal S6 kinase, and ribosomal S6 protein.Compared with XL147 alone, the combination exhibited a

    superior antitumor effect against trastuzumab-resistant tumor xenografts. Furthermore, treatment with XL147 and trastuzumab

    reduced the cancer stem-cell (CSC) fraction within trastuzumab-resistant cells both in vitro and in vivo.

    in vivo: SAR245408 induced significant differences in EFS distribution compared to control in 29 of 37 (79%) of solid tumor

    xenografts and in two of seven (29%) ALL. Xenografts. SAR245408 induced tumor growth inhibition meeting criteria for

    intermediate EFS T/C activity (EFS T/C?>?2) in 4 of 37 (11%) solid tumor xenografts.

    Toxicity: In vitro SAR245408 demonstrated cytotoxic activity, with a median relative IC50 value of 10.9??M (range

    2.7-24.5??M).

    Chemical Information

    Catalog DC8184

    Purity of current batch: >98%

    Molecular Weight (MW) 540.13

    Molecular Formula C25H25ClN6O4S

    CAS No. 934526-89-3

    Solubility (25C) DMSO

    Storage Store at -20C (desiccating conditions).

    Handling:

    Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.

    Website:www.dcchemicals.com

    Email: info@dcchemicals.com Phone:+86-21-58447131

    Marketing Center: Room 610,Building 15, Jinxiang Rd 201, Shanghai,

    China

  • Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in

    advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable

    for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room

    temperature for at least 1 hour.