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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.
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice.
| 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 |
| Molecular Weight | 851.96 |
| Formula | C44H47F2N9O5S |
| CAS Number | 1089283-49-7 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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