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Related PI3K Inhibitors
A66

A66 is a potent and specific inhibitor of PI3K p110α with IC50 values of 32, 30 and 43 nM for p110α, p110α/E545K and p110α/H1047R.

NU7441

NU7441 (KU 57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 values of 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.

TGX-221

TGX-221 is a potent and specific cell permeable inhibitor of Phosphatidylinositol 3-kinase (PI3K) p110β(IC50 = 10nM).

XL765

Cat. No. M1849

XL765 Structure

Synonym: SAR245409, XL-765

Size Price Availability Quantity
10mg $280 In stock
50mg $780 In stock
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Quality Control

  • Current batch:
  • Purity >98%
  • COA
  • MSDS

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.


Chemical Information

Molecular Weight 599.66
Formula C31H29N5O6S
CAS Number 1123889-87-1
Purity >98%
Solubility DMSO ≥15 mg/mL
Storage at -20°C

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.



Keywords: XL765, SAR245409, XL-765, supplier, potent, PI3K, kinases, inhibitors, inhibits

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