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Golvatinib (E7050) (C007B-173150)

Catalog No.
C007B-173150
Mfr. No.
G408315-1ml
Mfr. Name
Aladdin Scientific
Qty/UOM
1
UOM
EA
Price: $387.63
List Price: $430.70

InformationGolvatinib (E7050) is a dualc-MetandVEGFR-2inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.In vitroIn vitro studies indicate that E7050 potently inhibits phosphorylation of

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InformationGolvatinib (E7050) is a dualc-MetandVEGFR-2inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.In vitroIn vitro studies indicate that E7050 potently inhibits phosphorylation of both c-Met and VEGFR-2. E7050 also potently represses the growth of both c-met amplified tumor cells and endothelial cells stimulated with either HGF or VEGF. E7050 circumvents resistance to all of the reversible, irreversible, and mutant-selective EGFR-TKIs induced by exogenous and/or endogenous HGF in EGFR mutant lung cancer cell lines, by blocking the Met/Gab1/PI3K/Akt pathway in vitro. E7050 also prevents the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF.In vivoIn vivo studies using E7050 shows inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models. Treatment of some tumor lines containing c-met amplifications with high doses of E7050 (50–200 mg/kg) induces tumor regression and disappearance. In a peritoneal dissemination model, E7050 shows an antitumor effect against peritoneal tumors as well as a significant prolongation of lifespan in treated mice. In another xenograft model research, tumors produced by HGF-transfected Ma-1 (Ma-1/HGF) cells are more angiogenic than vector control tumors and shows resistance to ZD1839. E7050 alone inhibits angiogenesis and retards growth of Ma-1/HGF tumors. E7050 combined with ZD1839 induces marked regression of tumor growth.Cell Datacell lines:HMC-1 and COLO-205Concentrations:5-5000 nMIncubation Time:3 daysPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C33H37F2N7O4 Molecular Weight: 633.69
UPC:
51321808
Condition:
New
Availability:
2 weeks
Weight:
0.85 Ounces
HazmatClass:
No
WeightUOM:
LB
MPN:
G408315-1ml
CAS:
928037-13-2
Product Size:
1ml

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