Datasheet of XL-147
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
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).
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.
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