Voxtalisib (SAR245409, XL765) Analogue

Catalog No.S1523

Voxtalisib (SAR245409, XL765) Analogue Chemical Structure

Molecular Weight(MW): 599.66

Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.

Size Price Stock Quantity  
In DMSO USD 500 In stock
USD 210 In stock
USD 370 In stock
USD 970 In stock
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3 Customer Reviews

  • The TMZ/XL765 combination decreases serum GH and PRL of mice bearing GH3 xenografts. A and B, After treatment with DMSO, TMZ, XL765, or the XL765/TMZ combination, the blood of the nude mice xenograft with GH3 tumor was collected and serum rat-GH and rat-PRL were measured by IRMA (TMZ/XL765 combination vs TMZ or XL765 alone: ***P <.001).

    Endocrinology 2013 154, 1247-59. Voxtalisib (SAR245409, XL765) Analogue purchased from Selleck.

    TMZ, XL765, or the TMZ/XL765 combination treatment inhibits the cell proliferation and induces the cell apoptosis of GH3 cells in vivo. A and B, Ki-67 expression in the section of GH3 tumors treated with DMSO, TMZ, XL765, or the TMZ/XL765 combination was determined by IHC. Positive cells appear brown, whereas negative cells remain blue (n=10 tumors per group). Magnification, ?0 as indicated. CTRL, control. C and D , The apoptotic cells of tumor tissues from various treatments were detected by TUNEL staining. TUNEL-positive cells appear brown, whereas negative cells remain blue (n =10 tumors per group). Magnification, ?40 as indicated. (TMZ/XL765 combination vs TMZ or XL765 alone; *** P<0.001).

    Endocrinology 2013 154, 1247-59. Voxtalisib (SAR245409, XL765) Analogue purchased from Selleck.

  • After starved in serum-free medium for 24 h, A549 cells incubated with the indicated concentrations of XL765 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. Voxtalisib (SAR245409, XL765) Analogue purchased from Selleck.

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Biological Activity

Description Voxtalisib (SAR245409, XL765) Analogue 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] PI3Kα [1] PI3Kδ [1] PI3Kβ [1] DNA-PK [1]
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]

+ Expand
  • 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 12 mg/mL (20.01 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or 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 599.66
Formula

C31H29N5O6S

CAS No. 1349796-36-6
Storage powder
in solvent
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