1349796-36-6

Basic information

• Product Name: XL765
• Synonyms: SAR245409 (XL765);PI3K-IN-1;N-[4-[[[3-[(3,5-Dimethoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-3-methoxy-4-methylbenzamide;Benzamide, N-[4-[[[3-[(3,5-dimethoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-3-methoxy-4-methyl-;Voxtalisib (SAR245409, XL765);N-[4-[[[3-[(3,5-Dimethoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-3-methoxy-4-methylbenzamide SAR245409 (XL765);XL765 N-[4-[[[3-[(3,5-Dimethoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-3-methoxy-4-methylbenzamide;XL765, >=98%
• CAS NO: 1349796-36-6
• Molecular Formula: C31H29N5O6S
• Molecular Weight: 599.65686
• Product Categories: PI3K/Akt/mTOR;Inhibitors;Akt;mTOR;PI3K
• Mol File: 1349796-36-6.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.387±0.06 g/cm3(Predicted)
• Solubility: insoluble in H2O; insoluble in EtOH; ≥15 mg/mL in DMSO
• PKA: 5.88±0.30(Predicted)
• CAS DataBase Reference: XL765(CAS DataBase Reference)
• NIST Chemistry Reference: XL765(1349796-36-6)
• EPA Substance Registry System: XL765(1349796-36-6)

Safety Data

• Hazardous Substances Data: 1349796-36-6(Hazardous Substances Data)

Usage

Biological Activity

sar245409 (xl765) is a selective dual inhibitor of pi3k and mtor (ic50= 9 nm for pi3kγ).pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in pa cell lines, combination of xl765 and tmz blocked the cell growth and led to apoptosis [1]. in a variety of tumor cell lines that mutated on pi3k signaling, xl765 inhibited pip3 formation in the membrane and akt/p70s6k/s6 phosphorylation [2].in gh3 xenograft tumor mouse models, combination use of xl765 and tmz inhibited tumor growth, reduced serum gh and prolactin levels with no increased systemic side effects [1]. in severe combined immunodeficient mice, xl765 abolished mpnst local and metastatic growth. [3]. in multiple human xenograft models in nude mice, repeat dose administration showed significant tumor growth inhibition that related to antiproliferative and antiangiogenic response etc. [2]

references

1. dai c, zhang b, liu x et al. inhibition of pi3k/akt/mtor pathway enhances temozolomide-induced cytotoxicity in pituitary adenoma cell lines in vitro and xenografted pituitary adenoma in female nude mice. endocrinology. 2013 mar;154(3):1247-59.2. yu p, laird ad, du x et al. characterization of the activity of the pi3k/mtor inhibitor xl765 (sar245409) in tumor models with diverse genetic alterations affecting the pi3k pathway. molcancer ther. 2014 may;13(5):1078-91.3. ghadimi mp, lopez g, torres ke et al. targeting the pi3k/mtor axis, alone and in combination with autophagy blockade, for the treatment of malignant peripheral nerve sheath tumors. mol cancer ther. 2012 aug;11(8):1758-69.