AT-13148

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AT-13148

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Cat No: 21597

Biochemicals - Kinase Inhibitors

AT-13148 is an orally bioavailable and ATP-competitive multi-AGC kinase inhibitor.{38275} It inhibits Akt1, 2, and 3 (IC50s = 38, 402, and 50 nM, respectively), in addition to other AGC kinase family members p70S6K, PKA, ROCK1, and ROCK2 (IC50s = 3-8 ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(?S)-?-(aminomethyl)-?-(4-chlorophenyl)-4-(1H-pyrazol-4-yl)-benzenemethanol

Correlated keywords:

AT13148 Akt2 Akt3 ROCK-I ROCK-II BT-474 MLC-2 anti-proliferative ROCKI ROCKII

Product Overview:
AT-13148 is an orally bioavailable and ATP-competitive multi-AGC kinase inhibitor.{38275} It inhibits Akt1, 2, and 3 (IC50s = 38, 402, and 50 nM, respectively), in addition to other AGC kinase family members p70S6K, PKA, ROCK1, and ROCK2 (IC50s = 3-8 nM). AT-13148 inhibits growth of cancer cell lines with genetic mutations in PI3K-Akt-mTOR and RAS-RAF signaling pathways (GI50s = 1.54-3.77 μM). In vivo administration of AT-13148 (50 mg/kg, p.o.) inhibits the growth of MES-SA uterine sarcoma and BT474 breast cancer xenografts in mice by inhibiting Akt and p70S6K kinases. AT-13148 also stably inhibits ROCK-dependent phosphorylation of myosin light chain (MLC2) over a 24-hour period in 4599 mouse melanoma cells (EC50 = 0.1 μM).{38276} Oral administration at a dose of 40 mg/kg reduces motility of 4699 melanoma cells in murine xenograft model.

Size	1 mg
Shipping	dry ice
CAS Number	1056901-62-2
Molecular Formula	C₁₇H₁₆ClN₃O
SMILES	ClC1=CC=C([C@@](CN)(O)C2=CC=C(C3=CNN=C3)C=C2)C=C1
Molecular Weight	313,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.19
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.