XL147

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XL147

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Cat No: 18011

Biochemicals - Kinase Inhibitors

The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. XL147 is a methylbenzenesulfonamide derivative that reversibly inhibits class I PI3Ks (IC50s = 39, 36, 23, and 383 nM for p110α, δ, ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-amino-N-[3-[[[3-[(2-chloro-5-methoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-2-methyl-propanamide

Correlated keywords:

1033110-57-4 XL-147 SAR-245408 p110-? p110? p110? p110? Vps-34 XL-147 MCF7 PC-3 BT-474

Product Overview:
The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. XL147 is a methylbenzenesulfonamide derivative that reversibly inhibits class I PI3Ks (IC50s = 39, 36, 23, and 383 nM for p110α, δ, γ, and β, respectively).{29152} It has been shown to abrogate Akt and S6 kinase phosphorylation, reduce cyclin D1 and retinoblastoma protein, and upregulate the CDK inhibitor p27, inhibiting cell proliferation.{29152} In HER2-overexpressing breast cancer cells, cotreatment with the HER2 inhibitors trastuzumab or lapatinib (Item No. 11493) are reported to sensitize tumor cells to the growth inhibitory effect of XL147.{29153} This compound has been evaluated in clinical trials in patients with advanced solid tumors.{29154}

Size	5 mg
Shipping	dry ice
CAS Number	934526-89-3
Molecular Formula	C₂₅H₂₅ClN₆O₄S
SMILES	COC1=CC(NC2=NC3=CC=CC=C3N=C2NS(C4=CC=CC(NC(C(C)(N)C)=O)=C4)(=O)=O)=C(Cl)C=C1
Molecular Weight	541
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.49
UNSPSC code	12352100

Technical File

MSDS

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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.