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GDC-0623

GDC-0623 ??? ???
?? ??:
1168091-68-6
???:
GDC-0623
???(??):
G-868;CS-1791;RG 7421;GDC-0623;MEK inhibitor 1;GDC-0623 (G-868);GDC-0623, 10 mM in DMSO;5-((2-FLUORO-4-IODOPHENYL)AMINO)-N-(2-HYDROXYETHOXY)IMIDAZO[1,5-A]PYRIDINE-6-CARBOXAMIDE;Imidazo[1,5-a]pyridine-6-carboxamide, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-;5-(2-Fluoro-4-iodophenylamino)imidazo[1,5-a]pyridine-6-carboxylic acid N-(2-hydroxyethoxy)amide
CBNumber:
CB72655407
???:
C16H14FIN4O3
??? ??:
456.21
MOL ??:
1168091-68-6.mol

GDC-0623 ??

??
1.81±0.1 g/cm3(Predicted)
?? ??
Store at -20°C
???
insoluble in H2O; ≥16.85 mg/mL in DMSO; ≥2.69 mg/mL in EtOH with ultrasonic
??? ??
??
??? ??
??? ??
?? ?? (pKa)
14.17±0.10(Predicted)
??
Light yellow to gray
InChI
InChI=1S/C16H14FIN4O3/c17-13-7-10(18)1-4-14(13)20-15-12(16(24)21-25-6-5-23)3-2-11-8-19-9-22(11)15/h1-4,7-9,20,23H,5-6H2,(H,21,24)
InChIKey
RFWVETIZUQEJEF-UHFFFAOYSA-N
SMILES
C12=CN=CN1C(NC1=CC=C(I)C=C1F)=C(C(NOCCO)=O)C=C2
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
????(GHS): Exclamation Mark (GHS07)
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H302 ??? ??? ?? ?? ?? - ?? ?? 4 ?? P264, P270, P301+P312, P330, P501
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ??
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
2 0

GDC-0623 C??? ??, ??, ??

??

GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP). It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively. GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.

GDC-0623 ?? ?? ? ???

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?? ??


GDC-0623 ?? ??

???( 96)?? ??
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GDC-0623 ?? ??:

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