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????(E7050)

????(E7050)
????(E7050) ??? ???
?? ??:
928037-13-2
???:
????(E7050)
???(??):
????(E7050)
???:
Golvatinib (E7050)
???(??):
E-7050;E-7060;CS-575;Golvatinib;Golvatinib (E7050);E-7060;E7050;E 7050;E-7050 (Golvatinib);Golvatinib E7050 E-7050;Golvatinib, 10 mM in DMSO;Golvatinib (E7050) USP/EP/BP
CBNumber:
CB12589746
???:
C33H37F2N7O4
??? ??:
633.69
MOL ??:
928037-13-2.mol

????(E7050) ??

???
187 - 190°C
?? ?
867.5±65.0 °C(Predicted)
??
1.408
?? ??
Refrigerator
???
DMSO(?? ???), ???(?? ???)
??? ??
??
??? ??
??? ??
?? ?? (pKa)
12.91±0.70(Predicted)
??
???? ?????
CAS ??????
928037-13-2
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P271 ?? ?? ??? ? ?? ???? ?????.
P280 ????/???/???/?????? ?????.
P302+P352 ??? ??? ??? ?? ????.
P304+P340 ???? ??? ??? ?? ??? ??? ???? ?? ??? ??? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
P312 ???? ??? ????(??)? ??? ????.
P321 (…) ??? ???.
P332+P313 ?? ??? ??? ???? ??· ??? ????.
P337+P313 ?? ?? ??? ???? ???? ??· ??? ????.
P403+P233 ??? ??? ? ?? ?? ??? ???? ?????.
P405 ???? ?????.
P501 ...? ??? / ??? ?? ???.
NFPA 704
0
2 0

????(E7050) C??? ??, ??, ??

??

Golvatinib is an orally bioavailable dual inhibitor of the receptor tyrosine kinases c-Met and VEGF receptor 2 (VEGFR2), which are involved in tumor progression. Golvatinib inhibits autophosphorylation of c-Met in MKN45 cells and phosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50s = 14 and 16 nM, respectively). It also inhibits proliferation of a variety of cancer cell lines and of HUVECs stimulated with hepatocyte growth factor (HGF) and VEGF but not bFGF (IC50s = 17, 84, and >1,000 nM for HGF-, VEGF-, and bFGF-stimulated HUVECs, respectively). In nude mouse xenograft models using MKN45, Hs746T, SNU-5, or EBC-1 cancer cells, golvatinib (25-200 mg/kg, daily) dose-dependently reduces tumor volume, and it increases survival in the model using MKN45 cells.

??

E7050 is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, respectively.

????(E7050) ?? ?? ? ???

???

?? ??

????(E7050) ?? ??

???( 146)?? ??
??? ?? ??? ?? ?? ? ??
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????(E7050) ?? ??:

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