Voxtalisib (XL765, SAR245409)

Catalog No.S7646

Voxtalisib (XL765, SAR245409) Chemical Structure

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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Biological Activity

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.
Targets
PI3Kγ [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
DNA-PK [1]
(Cell-free assay)
9 nM 39 nM 43 nM 113 nM 150 nM
In vitro

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. [1] 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. [2]

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. [2] 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. [3]

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: Pancreatic cancer cell lines (HcG25, Panc89, PA-TU8988T, Panc2.13, MiaPaCa2, Panc10.05, Panc8.13, BxPC-3, etc.)
  • Concentrations: Dissolved in DMSO, final concentration ~10 μM
  • Incubation Time: 24, 48, 72 hours
  • Method:

    Cells are treated with XL765 24 hours after plating and harvested for apoptosis or autophagy assays at 24, 48, or 72 hours after XL765 treatment. Apoptosis is determined by total percentage of annexin V-positive cells by fluorescence-activated cell sorting (FACS). Acidic vesicular organelles (AVOs) are detected in XL765-treated cells by vital staining with acridine orange. The degree of AVO formation is expressed as fold increase of acridine orange fluorescence intensity (FL3) in XL765-treated cells versus control cells.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Female Nu/Nu mice inoculated s.c. with BxPC-3 cells
  • Formulation: Solubilized in water/10 mM HCl
  • Dosages: 30 mg/kg
  • Administration: Oral gavage once a day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 270.29
Formula

C13H14N6O

CAS No. 934493-76-2
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01936363 Active, not recruiting Ovarian Cancer EMD Serono|Sanofi September 2013 Phase 2
NCT01587040 Active, not recruiting Neoplasm Malignant Sanofi July 2012 Phase 1|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
NCT01390818 Completed Locally Advanced Solid Tumor|Metastatic Solid Tumor|Breast Cancer|Non Small Cell Lung Cancer|Melanoma|Colorectal Cancer EMD Serono|Sanofi May 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID