GSK1838705A

Confirm delete?

GSK1838705A

Zoom

Cat No: 24904

Biochemicals - Kinase Inhibitors

GSK1838705A is an inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) and the insulin receptor (IR; IC50s = 2 and 1.6 nM, respectively).{41768} It is selective for IGF-1R and IR over a panel of 47 kinases (IC50s = >1,600 nM), however, it a...

This product can only be bought through Cayman Chemical. Please contact us.

Product Overview
Data
Downloads
About Cayman

Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[[2-[[1-[2-(dimethylamino)acetyl]-2,3-dihydro-5-methoxy-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methyl-benzamide

Correlated keywords:

1116236-05-5 GSK-1838705-A 1838705A IGF1R IGF1 IGFIR IRS1 MCF7 COLO205 NIH3T2 LISN U-87-MG U87 87MG PC3-R

Product Overview:
GSK1838705A is an inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) and the insulin receptor (IR; IC50s = 2 and 1.6 nM, respectively).{41768} It is selective for IGF-1R and IR over a panel of 47 kinases (IC50s = >1,600 nM), however, it also inhibits anaplastic lymphoma kinase (ALK; IC50 = 0.5 nM). GSK1838705A inhibits IGF-1 and insulin-induced phosphorylation of IGF-1R and IR in a concentration-dependent manner as well as phosphorylation of the downstream signaling markers Akt, IRS-1, and ERK in MCF-7 breast carcinoma cells. It inhibits growth in a panel of cancer cell lines (EC50s = 24-8,378 nM) with the IGF-1R signaling-dependent multiple myeloma and Ewing's sarcoma cell lines being the most sensitive. In vivo, GSK1838705A completely inhibits IGF-1-induced phosphorylation of IGF-1R, Akt, and IRS-1 as well as reduces tumor growth in the COLO 205 and NIH-3T2/LISN mouse xenograft models when administered at doses of ≥1 and ≥10 mg/kg, respectively. It also induces tumor cell apoptosis and reduces tumor growth in U87MG glioma and PC3R prostate cancer mouse xenograft models.{41769,41770}

Size	5 mg
Shipping	dry ice
CAS Number	1116235-97-2
Molecular Formula	C₂₇H₂₉FN₈O₃
SMILES	FC1=CC=CC(NC2=C(C=CN3)C3=NC(NC4=CC(N(C(CN(C)C)=O)CC5)=C5C=C4OC)=N2)=C1C(NC)=O
Molecular Weight	532,6
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2903.99
UNSPSC code	12352100

Technical File

MSDS

Click here to ask for your quote and get 15% off Cayman's products.

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.