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Tyrosine Kinase/Adaptors IGF-1R GSK1904529A

GSK1904529A

Catalog No. T6003   CAS 1089283-49-7
Synonyms: GSK 4529, GSK 4529

GSK1904529A is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

GSK1904529A, CAS 1089283-49-7
Pack Size Availability Price/USD Quantity
2 mg In stock 52.00
5 mg In stock 90.00
10 mg In stock 126.00
25 mg In stock 196.00
50 mg Inquiry 315.00
100 mg Inquiry 567.00
1 mL * 10 mM (in DMSO) Inquiry 119.00
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Purity 98.64%
Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK1904529A is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
Targets&IC50 B-Raf (V600E) ,   IGF-1R ,   Insulin Receptor ,   Syk ,   VEGFR2
Kinase Assay 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 Research
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.</(Only for Reference)
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.
Synonyms GSK 4529 , GSK 4529
Purity 98.64%
Molecular Weight 851.96
Formula C44H47F2N9O5S
CAS No. 1089283-49-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 114 mg/mL (133.8 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Sabbatini P, et al. Clin Cancer Res, 2009, 15(9), 3058-3067.

Related compound libraries

This product is contained In the following compound libraries:
Fluorochemical Library

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