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XL-147 is an inhibitor of PI3K that is currently in clinical trials as a potential treatment for cancers with solid tumors. XL-147 exhibits anticancer chemotherapeutic properties, inhibiting tumor growth in animal models of acute lymphocytic leukemia (ALL). XL-147 is a dual inhibitor of PI3K and mTOR. It exhibits higher efficacy than either sole PI3K or mTOR inhibition in models of prostate cancer.
| Cas No. | 934526-89-3 |
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| Purity | ≥98% |
| Formula | C25H25ClN6O4S |
| Formula Wt. | 541.02 |
| IUPAC Name | N-[3-(2,1,3-benzothiadiazol-5-ylamino)quinoxalin-2-yl]-4-methylbenzenesulfonamide |
| Synonym | Pilaralisib, SAR245408 |
| Solubility | DMSO 3 mg/mL (6.68 mM) Water Insoluble Ethanol Insoluble |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Shapiro GI, Rodon J, Bedell C, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2014 Jan 1;20(1):233-45. PMID: 24166903.
Reynolds CP, Kang MH, Carol H, et al. Initial testing (stage 1) of the phosphatidylinositol 3' kinase inhibitor, SAR245408 (XL147) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2013 May;60(5):791-8. PMID: 23002019.
Gravina G., Mancini A., Dual PI3K/mTOR inhibitor, XL765 (SAR245409), shows superior effects to sole PI3K [XL147 (SAR245408)] or mTOR [rapamycin] inhibition in prostate cancer cell models. 37(1):341-51 (2016). PMID: 26219891.
