XL-147
| CAS No. | 934526-89-3 | Cat. No. | BCP15312 |
| Name | XL-147 | ||
| Synonyms | SAR245408;XL 147;XL147;SAR-245408;SAR 245408;Pilaralisib; | ||
| Formula | C25H25ClN6O4S | M. Wt | 541.02 |
| Description | 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 [1].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%) so | ||
| Pathways | PI3K/Akt/mTOR | ||
| Targets | PI3K | ||
Structure
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