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Cat. No. M1849

XL765 Structure

Synonym: SAR245409, XL-765

Size Price Availability Quantity
10mg $280 In stock
50mg $680 In stock
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Quality Control
Biological Activity

XL765 (SAR245409) is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. XL765 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in susceptible tumor cell populations. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy. mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion in response to nutrient and energy deprivation. 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. In preclinical studies, XL765 slowed tumor growth or caused tumor shrinkage in multiple preclinical cancer models, including breast, lung, ovarian, prostate cancers, and gliomas.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 599.66
Formula C31H29N5O6S
CAS Number 1123889-87-1
Purity 100.00%
Solubility DMSO ≥15 mg/mL
Storage at -20°C
Chemical Name N-[4-[[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-3-methoxy-4-methylbenzamide

Targeting the PI3K/mTOR Axis, Alone and in Combination with Autophagy Blockade, for the Treatment of Malignant Peripheral Nerve Sheath Tumors.
Ghadimi et al. Mol Cancer Ther. 2012 Aug;11(8):1758-69. PMID: 22848094.

Autophagy suppression promotes apoptotic cell death in response to inhibition of the PI3K-mTOR pathway in pancreatic adenocarcinoma.
Mirzoeva et al. J Mol Med (Berl). 2011 Sep;89(9):877-89. PMID: 21678117.

Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide.
Prasad et al. Neuro Oncol. 2011 Apr;13(4):384-92. PMID: 21317208.

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Keywords: XL765, SAR245409, XL-765 supplier, PI3K, inhibitors

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