3137385-11-3
Chemical Structure
KRAS-IN-62
- CAS No.: 3137385-11-3
- Formula:C35H34F7N9O3
- Molecular Weight:761.69
InChIKey: NGQDCQGUIAPWMJ-BJSPTKCDSA-N
SMILES: FC(F)(F)C(C(C)=CC1=C2C=NN1)=C2C3=C(F)C4=C(C(OC[C@H](C)N5[C@H](C)C6=C(N)N=CC(OC(F)F)=C6)=N3)C5=NC(OC[C@@]78N(CCC8)C[C@H](F)C7)=N4
Biological Activity: KRAS-IN-62 is an orally effective pan-KRAS inhibitor that potently inhibits SOS1-mediated KRAS nucleotide exchange (IC50 < 10 nM for KRAS G12D/G12V/G12C/WT). KRAS-IN-62 inhibits pERK signaling and cell proliferation in KRAS-mutant tumor cells (pERK IC90 = 0.51 nM in GP2D cells). KRAS-IN-62 inhibits tumor growth in vivo, with plasma concentrations exceeding IC50 for ~20 h after oral administration in beagle dogs. KRAS-IN-62 can be used in studies of KRAS mutation-related cancers, such as colorectal cancer[1].
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KRAS-IN-62 | KRAS-IN-62 is an orally effective pan-KRAS inhibitor that potently inhibits SOS1-mediated KRAS nucleotide exchange (IC50 < 10 nM for KRAS G12D/G12V/G12C/WT). KRAS-IN-62 inhibits pERK signaling and cell proliferation in KRAS-mutant tumor cells (pERK IC90 = 0.51 nM in GP2D cells). KRAS-IN-62 inhibits tumor growth in vivo, with plasma concentrations exceeding IC50 for ~20 h after oral administration in beagle dogs. KRAS-IN-62 can be used in studies of KRAS mutation-related cancers, such as colorectal cancer. | |||||||||||||||||||||
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Keywords
