Introduction：Basic information about CAS 1089283-49-7|GSK1904529A, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | GSK1904529A |
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| CAS Number | 1089283-49-7 | Molecular Weight | 851.963 |
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| Density | 1.4±0.1 g/cm3 | Boiling Point | / |
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| Molecular Formula | C44H47F2N9O5S | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide |
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| Synonym | More Synonyms |
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GSK1904529A BiologicalActivity
| 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. IC50 value: 27/25 nM (IGF1R/IR) [1]Target: IGF1R/IRin 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]. |
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| Related Catalog | Signaling Pathways >>Protein Tyrosine Kinase/RTK >>IGF-1RResearch Areas >>Cancer |
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| References | [1]. Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res, 2009, 15(9), 3058-3067. |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Molecular Formula | C44H47F2N9O5S |
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| Molecular Weight | 851.963 |
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| Exact Mass | 851.338867 |
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| PSA | 158.40000 |
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| LogP | 4.69 |
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| Index of Refraction | 1.672 |
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| InChIKey | MOSKATHMXWSZTQ-UHFFFAOYSA-N |
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| SMILES | CCc1cc(Nc2nccc(-c3c(-c4ccc(OC)c(C(=O)Nc5c(F)cccc5F)c4)nc4ccccn34)n2)c(OC)cc1N1CCC(N2CCN(S(C)(=O)=O)CC2)CC1 |
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| Storage condition | -20℃ |
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Synonyms
| gsk1904529a |
| N-(2,6-Difluorophenyl)-5-(3-{2-[(5-ethyl-2-methoxy-4-{4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl}phenyl)amino]-4-pyrimidinyl}imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide |
| Benzamide, N-(2,6-difluorophenyl)-5-[3-[2-[[5-ethyl-2-methoxy-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-methoxy- |
