Voxtalisib

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Voxtalisib

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Cat No: 30323

Biochemicals - Kinase Inhibitors

Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)-pyrido[2,3-d]pyrimidin-7(8H)-one

Correlated keywords:

1070896-79-5 1123889-87-1 1380852-52-7 PI3K ? ? ? ? mTORC 1 2 VPS 34 DNAPK PIP 2 PC 3 S6 RP GBM39 XL 765 SAR 245409

Product Overview:
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}

Size	5 mg
Shipping	dry ice
CAS Number	934493-76-2
Molecular Formula	C₁₃H₁₄N₆O
SMILES	NC1=NC(C)=C(C=C(C2=NNC=C2)C(N3CC)=O)C3=N1
Molecular Weight	270,3
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.79
UNSPSC code	12352100

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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.