Voxtalisib (XL765, SAR245409)
Molecular Weight(MW): 270.29
Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
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Cell viability measurements. The IMR-32, LA-N-1 and CHP‑134 cells were treated with mTOR/PI3K inhibitor SAR245409 alone or in combination with the 14G2a mAb (40 μg/ml) for 72 h. The cell viability was determined by measuring ATP content, and compared to respective controls treated with appropriate diluents (DMSO or water, set as 1). P-values for t-test were as follows: *p<0.05, **p<0.01, ***p<0.001.
Int J Oncol, 2015, 47(3):1143-59. . Voxtalisib (XL765, SAR245409) purchased from Selleck.
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Choose Selective PI3K Inhibitors
|Description||Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.|
XL765 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ, respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM.  XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL765, a dual-target PI3K/mTOR inhibitor, inhibits cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90. The effect can be recapitulated by using combinations of single-targeted compounds. XL765 significantly reduces phosphorylation of the mTOR targets S6, S6K, and 4EBP1, which is associated with greater apoptosis induction rather than to PI3K inhibition alone. XL765 treatment causes accumulation of autophagosomes in MIAPaCa-2 cells, and results in significant dose-dependent AVO induction and LC3-II stimulation in MIAPaCa-2 cells stably expressing a LC3-GFP construct. 
|In vivo||The combination of XL765 (30 mg/kg) with chloroquine (50 mg/kg) results in significant inhibition of BxPC-3 xenograft growth in mice models, while XL765 alone at the same dose has no inhibitory effect.  Oral administration of XL765 results in greater than 12-fold reduction in median tumor bioluminescence compared to control and improvement in median survival in nude mice implanted intracranially with GBM 39-luc cells. XL765 in combination with temozolomide (TMZ) yields a 140-fold reduction in median bioluminescence with a trend toward improvement in median survival compared with TMZ alone. |
|In vitro||DMSO||54 mg/mL (199.78 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01936363||Completed||Ovarian Cancer||EMD Serono|Sanofi||September 30 2013||Phase 2|
|NCT01596270||Completed||Neoplasm Malignant||Sanofi||June 2012||Phase 1|
|NCT01410513||Completed||Indolent Non-Hodgkin Lymphoma|Mantle Cell Lymphoma|Chronic Lymphocytic Leukemia||Sanofi||December 2011||Phase 1|
|NCT01403636||Completed||Lymphoma||Sanofi||October 2011||Phase 2|
|NCT01240460||Completed||Glioblastoma|Astrocytoma Grade IV||Sanofi||January 2011||Phase 1|
|NCT01082068||Completed||Breast Cancer||Sanofi||June 2010||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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