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GSK-2126458

GSK-2126458 ??? ???
?? ??:
1086062-66-9
???:
GSK-2126458
???(??):
CS-55;GSK458;GSK212;HYR-582;OMipalisib;GSK2126458;GSK-2126458;GSK-2126458-A;GSK2126458, >=98%;Omipalisib GSK458
CBNumber:
CB92505205
???:
C25H17F2N5O3S
??? ??:
505.5
MOL ??:
1086062-66-9.mol
MSDS ??:
SDS

GSK-2126458 ??

???
187-189℃
?? ?
715.6±70.0 °C(Predicted)
??
1.45
?? ??
Refrigerator
???
????? (?? ???), DMSO (?? ???), ???(?? ??, ??)
??? ??
??
??? ??
??? ??
?? ?? (pKa)
6.23±0.40(Predicted)
??
???? ?? ???
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
HS ?? 29350090
????(GHS): GHS hazard pictogramsGHS hazard pictograms
?? ?: Danger
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H302 ??? ??? ?? ?? ?? - ?? ?? 4 ?? GHS hazard pictograms P264, P270, P301+P312, P330, P501
H372 ??? ?? ?? ???? ??(??, ??? ?? ??? ?? ??? ??)? ??? ??? ?? ???? ?? - ?? ?? ?? 1 ?? GHS hazard pictograms P260, P264, P270, P314, P501
??????:
P202 ?? ?? ?? ??? ?? ???? ??? ???? ???.
P260 ??·?·??·???·??·...·????? ???? ???.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P270 ? ??? ??? ??? ???, ???? ???? ???.
P301+P312 ??? ???? ??? ????(??)? ??? ????.
P308+P313 ?? ?? ??? ???? ???? ??· ??? ????.
NFPA 704
0
2 0

GSK-2126458 C??? ??, ??, ??

??

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively). It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several common mutant forms of p110α. GSK2126458 is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models. GSK2126458 positively combines with inhibitors of discoidin domain receptor 1 (DDR1) inhibitor DDR1-IN-1 to suppress the growth of SNU-1040 colorectal cancer cells.

??

A highly potent inhibitor of PI3K and the mammalian target of Rapamycin.

GSK-2126458 ?? ?? ? ???

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GSK-2126458 ?? ??

???( 181)?? ??
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Capot Chemical Co.,Ltd.
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Hefei Hirisun Pharmatech Co., Ltd
+8615056975894
shawn@hirisunpharm.com CHINA 9911 58

GSK-2126458 ?? ??:

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