| Identification | Back Directory | [Name]
XL765 | [CAS]
1349796-36-6 | [Synonyms]
CS-1849
PI3K-IN-1
XL765, >=98%
Voxtalisib-Analog
SAR245409 (XL765)
Voxtalisib Analogue
Voxtalisib (SAR245409, XL765)
SAR245409; XL-765;SAR 245409;SAR- 245409
PI3K-IN-1 ;SAR245409;XL-765;SAR 245409;SAR- 245409
Voxtalisib analogue, 98%, a potent inhibitor of PI3K
N-(4-(N-(3-((3,5-Dimethoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-3-methoxy-4-methylben
N-{4-[3-(3,5-Dimethoxy-phenylamino)-quinoxalin-2-ylsulfamoyl]-phenyl}-3-methoxy-4-methyl-benzamide
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-
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 | [Molecular Formula]
C31H29N5O6S | [MDL Number]
MFCD18252649 | [MOL File]
1349796-36-6.mol | [Molecular Weight]
599.66 |
| Chemical Properties | Back Directory | [density ]
1.387±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥15 mg/mL in DMSO | [form ]
solid | [pka]
5.88±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
XL765 is a low-molecular mass PI3K inhibitor that also inhibits DNA-PK and mTOR. | [Definition]
ChEBI: XL765 is a sulfonamide obtained by formal condensation of the sulfonic acid group of 4-[(3-methoxy-4-methylbenzoyl)amino]benzenesulfonic acid with the primary aromatic amino group of N-(3,5-dimethoxyphenyl)quinoxaline-2,3-diamine. A dual PI3K/mTOR inhibitor used in cancer treatment. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, an antineoplastic agent and a mTOR inhibitor. It is a sulfonamide, a quinoxaline derivative, an aromatic amine, a member of benzamides and an aromatic ether. | [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] | [IC 50]
PI3K | [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. |
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