XL765
XL765 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
- SAR245409; XL-765;SAR 245409;SAR- 245409
- CAS:
- 1349796-36-6
- MF:
- C31H29N5O6S
- MW:
- 599.66
- Product Categories:
-
- Akt
- mTOR
- PI3K/Akt/mTOR
- Inhibitors
- PI3K
- Mol File:
- 1349796-36-6.mol
XL765 Chemical Properties
- 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
XL765 Usage And Synthesis
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]
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.
XL765Supplier
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- sales@boylechem.com
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