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GSK1904529A

Cat. No. M1717

GSK1904529A Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 210 In stock
50mg USD 520 In stock
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Quality Control
Biological Activity

GSK1904529A, selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. It is a promising candidate for therapeutic use in solid and hematologic cancers. IC50s for GSK1904529A in tumor cell lines ranged from 35 nmol/L to >30 umol/L. The tumor histologic types showing the greatest sensitivity to this compound were Ewing’s sarcoma and multiple myeloma, where IC50s in three of five Ewing’s sarcoma cell lines were <100 nmol/L and IC50s in five of eight multiple myeloma cell lines were <200 nmol/L.

Protocol
Cell Experiment
Cell lines NCI-H929, NIH-3T3/LISN, COLO 205, HT29, and BxPC3 cells
Preparation method Cell proliferation assays.
Cells were seeded in 96-well dishes, incubated overnight at 37°C, and treated with various concentrations of GSK1904529A for 72 h. For the NIH-3T3/LISN proliferation assays, cells were seeded on collagen-coated 96-well tissue culture plates (BD Biosciences) and allowed to adhere for 24 h. The tissue culture medium was replaced with serum-free medium and the cells were treated with DMSO or GSK1904529A for 2 h. IGF-I (30 ng/mL) was added and the cells were incubated at 37°C for 72 h. Cell proliferation was quantified using the CellTiter-Glo Luminescent Cell Viability Assay (Promega) following the manufacturer's recommendations. IC50 values were determined by using a four-parameter curve fit software package (XLfit4).
Concentrations 0~20 μM
Incubation time 72 h
Animal Experiment
Animal models NIH-3T3/LISN, COLO 205, HT29, and BxPC3 cells tumour xenograft model in female nu/nu CD-1 athymic mice
Formulation formulated in 20% sulfobutylether-β-cyclodextrin (pH 3.5; ISP)
Dosages 30 mg/kg once or twice daily for 21 d
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 851.96
Formula C44H47F2N9O5S
CAS Number 1089283-49-7
Purity >99%
Solubility DMSO 120 mg/mL
Storage at -20°C
References

Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
Sabbatini et al. Clin Cancer Res. 2009 May 1;15(9):3058-67. PMID: 19383820.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK1904529A supplier, IGF-1R, inhibitors

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