| Identification | Back Directory | [Name]
K-Ras G12C-IN-4 | [CAS]
2376328-55-9 | [Synonyms]
K-Ras G12C-IN-4
1H-Indole-1-acetamide, 5-chloro-2-cyclopropyl-3-[(3,4-dihydro-5-methoxy-2(1H)-isoquinolinyl)carbonyl]-7-methyl-N-[1-(1-oxo-2-propen-1-yl)-3-azetidinyl]- | [Molecular Formula]
C31H33ClN4O4 | [MDL Number]
MFCD32263400 | [MOL File]
2376328-55-9.mol | [Molecular Weight]
561.07 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 62.5 mg/mL (111.39 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C[1].
K-Ras G12C-IN-4 (4 hours) exhibits IC50=0.219 μM for inhibition of MAPK signaling (p-ERK) in MIA PaCa-2 cells[1].K-Ras G12C-IN-4 (72 hours) translates to a 0.067 μM IC50 for inhibition of cellular viability in a CellTiter-Glo experiment in MIA PaCa-2 cells[1]. | [References]
[1]. Shin Y, et al. Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C. ACS Med Chem Lett. 2019 Aug 20;10(9):1302-1308. |
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