GSK1904529A

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.

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GSK1904529A Chemical Structure

GSK1904529A Chemical Structure
Molecular Weight: 851.96

Validation & Quality Control

Customer Reviews(3)

Quality Control & MSDS

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Product Information

  • Inhibition Profile
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  • Research Area

Product Description

Biological Activity

Description GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
Targets Insulin Receptor [1] IGF-1R [1] B-Raf (V600E) [1] Syk [1] VEGFR2 [1]

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IC50 25 nM 27 nM >2 μM 3.2 μM 3.2 μM
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]
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

[1] Sabbatini P, et al. Clin Cancer Res, 2009, 15(9), 3058-3067.

Chemical Information

Download GSK1904529A SDF
Molecular Weight (MW) 851.96
Formula

C44H47F2N9O5S

CAS No. 1089283-49-7
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 124 mg/mL (145 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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

Research Area

Customer Reviews (3)


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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

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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.

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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 (3)

Tech Support & FAQs

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