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GSK1904529A

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, respectively.

Catalog No.S1093
5 5 3 Reviews 1 Product Citations
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GSK1904529A Chemical Structure

GSK1904529A Chemical Structure
Molecular Weight: 851.96

Validation & Quality Control

Product Citations(1)

Customer Reviews(3)

Quality Control & MSDS

Related Compound Libraries

GSK1904529A is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

Product Information

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  • Research Area

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, respectively.
Targets

IGF-1R

IR
IC50

27 nM

25 nM [1]
In vitro GSK1904529A is a reversible, ATP-competitive inhibitor and has enzyme-inhibitor binding values against IGF-1R and IR with Ki of 1.6 nM and 1.3 nM, respectively. GSK1904529A potently inhibits the ligand-induced phosphorylation of IGF-1R and IR at concentrations above 0.01 μM, followed by blocking downstream signaling (AKT, IRS-1, and ERK). GSK1904529A potently inhibits NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES RD-ES cells with IC50 of 60 nM, 35 nM, 43 nM, 61 nM and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines including NCI-H929, MOLP-8, LP-1 and KMS-12-BM etc. GSK1904529A induces cell cycle arrest at the G1 phase in cell lines COLO 205, MCF-7, and NCI-H929, which are sensitive to GK1904529A. [1]
In vivo GSK1904529A indicates 98% tumor growth inhibition in NIH-3T3/LISN tumor-bearing mice at a dose of 30 mg/kg (orally, twice-daily) and 75% in COLO 205 xenografts mice (once daily). Among HT29 and BxPC3 xenografts, GSK1904529A produces moderate tumor growth inhibition with no side effects at a dose of 30 mg/kg. Meanwhile, GSK1904529A shows minimal effects on blood glucose levels. GSK1904529A (~3.5 μM in blood) completely inhibits IGF-1R phosphorylation. GSK1904529A has been implicated in treatment of various IGF-1R-dependent tumors including prostate, colon, breast, pancreatic, ovarian, and sarcomas. [1]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

Kinase assays GSK1904529A is dissolved in DMSO as stock solution at 10 mM. Baculovirus-expressed glutathione S-transferase-tagged proteins encoding the intracellular domain of IGF-1R (amino acids 957-1367) and IR (amino acids 979-1382) are used for determination of IC50. Kinases are activated by preincubating the enzyme (2.7 μM final concentration) in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1mg/mL bovine serum albumin, and 2 mM ATP. GSK1904529A is diluted in DMSO and dispensed into the assay plates (100 nL/well). Kinase reactions contained (in 10 μL) 50 mM HEPES (pH 7.5), 3 mM DTT, 0.1mg/mL bovine serum albumin, 1mM CHAPS, 10 mM MgCl2, 10 μM ATP, 500 nM substrate peptide (biotin-aminohexylAEEEEYMMMMAKKKK-NH2; QPC), and 0.5 nM activated enzyme. Reactions are stopped after 1 hour at room temperature with 33 μM EDTA. Peptide phosphorylation is measured by time-resolved fluorescence resonance energy transfer with 7 nM streptavidin Surelight allophycocyanin and 1nM europium-conjugated phosphotyrosine antibodies. Plates are read in a multilabel reader.

Cell Assay:

[1]

Cell lines Tumor cell lines including multiple myeloma, ewing's sarcoma, askin's tumor, colon, breast, anaplastic large cell lymphoma, lung, cervix, head and neck, prostate and ovary.
Concentrations ~ 100 μM, stocked in DMSO at 10 mM.
Incubation Time 72 hours
Method

Cells are seeded in 96-well plates and incubated overnight at 37 °C, and treated with various concentrations of GSK1904529A for 72 hours. For the NIH-3T3/LISN, cells are seeded on collagen-coated 96-well tissue culture plates and allowed to adhere for 24 hours. The tissue culture medium is replaced with serum-free medium and the cells are treated with DMSO or GSK1904529A for 2 hours. IGF-I (30 ng/mL) is added and the cells are incubated at 37 °C for 72 hours. Cell proliferation is quantified using the CellTiter-Glo Luminescent Cell Viability Assay. IC50 values are determined.

Animal Study:

[1]

Animal Models NIH-3T3/LISN, COLO 205, HT29, and BxPC3 cells are implanted s.c. into the right flank of 8- to 10-wk-old female nu/nu CD-1athymic mice.
Formulation Formulated in 20% sulfobutylether-h-cyclodextrin (pH 3.5; ISP)
Dosages ~30 mg/kg
Administration Orally administered
1

References

Chemical Information

Download GSK1904529A SDF
Molecular Weight (MW) 851.96
Formula

C44H47F2N9O5S
CAS No. 1089283-49-7
Synonyms N/A
Solubility (25°C)
  • DMSO 124 mg/mL
  • Water <1 mg/mL
  • Ethanol <1 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)H-imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide
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Research Area

Customer Reviews (3)


Click to enlarge 		Rating
Source Dr. Ursula Broder from Institut. GSK1904529A purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 5 μM
Incubation Time 4 h
Results Inhibition of IGF-1 induced IGF-1R phosphorylation by GSK1904529A

Click to enlarge 		Rating
Source One customer. GSK1904529A purchased from Selleck
Method Cell growth inhibition assay
Cell Lines Melanoma cell lines
Concentrations 0.00000512-10 μM
Incubation Time 72 h
Results GSK1904529A treatment inhibited Melanoma cells growth in a does-dependent manner.

Click to enlarge 		Rating
Source Xuejun Jiang from Memorial Sloan-Kettering Cancer Center. GSK1904529A purchased from Selleck
Method Western blot
Cell Lines Mouse embryonic fibroblasts
Concentrations 5 μM
Incubation Time 1 h
Results GSK1904529A treatment resulted in a reduction of IGF-1R, IRS-1 and ERK1/2 phosphorylation.

Product Citations (1)

  • BRCA1 negatively regulates IGF-1 expression through an estrogen-responsive element-like site. [Kang HJ, et al. Cell Death Dis 2012;3, e336]

    PubMed: 22739988

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions
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