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XL388 is an orally bioavailable and ATP-competitive inhibitor of mammalian target of rapamycin (mTOR; IC50 = 9.9 nM).{42465} It is selective for mTOR over a panel of more than 140 kinases, including various PI3Ks (IC50s = >3,000 nM). It inhibits mTOR complex 1 (mTORC1) and mTORC2 in vitro (IC50s = 8 and 166 nM, respectively).{42466} XL388 induces cytotoxicity in MG-63, U2OS, and Saos-2 osteosarcoma and 786-0 kidney cancer cells and increases apoptosis in 786-0 and MG-63 cells in a concentration-dependent manner.{31720,42467} It also induces cell cycle arrest at the G1 phase and increases autophagy in MG-63 cells.{31720} XL388 (50 and 100 mg/kg) reduces tumor growth in an MCF-7 breast cancer mouse xenograft model and inhibits phosphorylation of the mTORC1 and mTORC2 substrates p70S6K, S6, 4E-BP1, and Akt in MCF-7 and PC-3 xenograft tumors when administered at a dose of 100 mg/kg.{42465} XL388 (20 mg/kg) also reduces tumor growth in U2OS and 786-0 mouse xenograft models.{31720,42467}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 10 mg, 25 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1251156-08-7 |
| Molecular formula | C23H22FN3O4S |
| Smiles | NC1=NC=C(C2=CC(CN(C(C3=C(C)C(F)=C(S(C)(=O)=O)C=C3)=O)CCO4)=C4C=C2)C=C1 |
| Molecular weight | 455,5 |
| Custom code | 2933.39 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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