Inhibitors, Agonists, Screening Libraries
Data Sheet
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Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kina inhibitor (TKI ) with IC 50s of 6.7, 1.9 and <1.0 nM for c-Met , VEGFR2 and Axl , respectively.
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In Vitro: Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kina inhibitor (TKI) with IC 50s of 6.7, 1.9 and <1.0nM for c-Met, VEGFR2 and Axl, respectively. In cell-bad functional assays, Ningetinib Tosylate (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC 50 values of 8.6 and 6.3 nM, respectively [1]. In Vivo: When single dod orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib Tosylate (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinas AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib Tosylate prolongs the median survival time (MST) and yields significant increa in life-span value (ILS=32%, p=0.003) at an oral do of 20 mg/kg/day (dod 21 days) versus the vehicle-treated group [1]. References:圣躬安
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[1]. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppress angiogenesis and tumor growth. Cancer Res 2014;74(19 Suppl):Abstract nr 1755.
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Product Name:
Ningetinib Tosylate Cat. No.:
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1394820-77-9Molecular Formula:
C 38H 37FN 4O 8S Molecular Weight:
728.79Target:
c-Met/HGFR; TAM Receptor; VEGFR Pathway:
Protein Tyrosine Kina/RTK Solubility:
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DMSO: 8.25 mg/mL
Caution: Product has not been fully validated for medical applications. For rearch u only.
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