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XL-765 is an inhibitor of PI3K and mTOR that displays anticancer chemotherapeutic and anti-angiogenic activities; it is currently in clinical trials as a potential treatment for lymphomas and solid tumors. XL-765 inhibits cell proliferation, tumor growth, and angiogenesis in cellular and animal models of cancers.
| Cas No. | 934493-76-2 |
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| Purity | ≥98% |
| Formula | C13H14N6O |
| Formula Wt. | 270.29 |
| IUPAC Name | 2-Amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7(8H)-one |
| Synonym | XL765, Voxtalisib, SAR245409 |
| Solubility | DMSO 12 mg/mL (20.01 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Light yellow powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Papadopoulos KP, Egile C, Ruiz-Soto R, et al. Efficacy, safety, pharmacokinetics and pharmacodynamics of SAR245409 (voxtalisib, XL765), an orally administered phosphoinositide 3-kinase/mammalian target of rapamycin inhibitor: a phase 1 expansion cohort in patients with relapsed or refractory lymphoma. Leuk Lymphoma. 2014 Nov 19:1-8. [Epub ahead of print] PMID: 25300944.
Yu P, Laird AD, Du X, et al. Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway. Mol Cancer Ther. 2014 May;13(5):1078-91. PMID: 24634413.
Papadopoulos KP, Tabernero J, Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245409 (XL765), a novel, orally administered PI3K/mTOR inhibitor in patients with advanced solid tumors. Clin Cancer Res. 2014 May 1;20(9):2445-56. PMID: 24583798.