| Identification | Back Directory | [Name]
BAY-293 | [CAS]
2244904-70-7 | [Synonyms]
BAY-293
BAY-293;BAY 293;BAY293
(R)-6,7-dimethoxy-2-methyl-N-(1-(4-(2-((methylamino)methyl)phenyl)thiophen-2-yl)ethyl)quinazolin-4-amine
4-Quinazolinamine, 6,7-dimethoxy-2-methyl-N-[(1R)-1-[4-[2-[(methylamino)methyl]phenyl]-2-thienyl]ethyl]-
(R)-(6,7-Dimethoxy-2-methyl-quinazolin-4-yl)-[1-[4-(2-methylaminomethyl-phenyl)-thiophen-2-yl]-ethyl]-amine | [Molecular Formula]
C25H28N4O2S | [MDL Number]
MFCD31813755 | [MOL File]
2244904-70-7.mol | [Molecular Weight]
448.58 |
| Chemical Properties | Back Directory | [Boiling point ]
553.4±50.0 °C(Predicted) | [density ]
1.218±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
9.61±0.10(Predicted) | [color ]
White to light yellow | [Optical Rotation]
[α]/D -85.0 to -103.0°, c =1.0 in DMSO | [InChIKey]
WEGLOYDTDILXDA-OAHLLOKOSA-N | [SMILES]
N1=C2C(C=C(OC)C(OC)=C2)=C(N[C@@H](C2SC=C(C3=CC=CC=C3CNC)C=2)C)N=C1C |
| Hazard Information | Back Directory | [Uses]
6,7-Dimethoxy-2-methyl-N-[(1R)-1-[4-[2-[(methylamino)methyl]phenyl]-2-thienyl]ethyl]-4-quinazolinamine is an effective and selective inhibitor of SOS1, blocking RAS activation via disruption of the KRAS-SOS1 interaction without significantly targeting the EGFR receptor. Thus, it has potential use in treatment of hyperproliferative disorders. | [Biological Activity]
BAY-293 selectively inhibits SOS1-mediated KRAS activation (IC50 = 52 nM; 50 nM wt or G12C hKRAS & 10 nM SOS1cat) via direct SOS1 bindingblocking SOS1-KRAS interaction (IC50 = 21 nM; 10 nM hSOS1c at & 5 nM hKRAS G12C) without affecting (IC50 >20 μM) CRAF RBD-KRAS interactionKRAS G12C activation by SOS2Cdc42 activation by DBSor EGFR kinase activity. BAY-293 downregulates cellular active RAS (IC50 = 200 nM/Calu-1410 nM/HeLa) and downstream ERK phosphorylation (K-562150 nM/Calu-1) with good target selectivity as assessed over 358 kinases (<37% inhibition at 1 μM) and a panel of 77 GPCRstransportersnuclear receptors and enzymes. | [IC 50]
KRAS-SOS1: 21 nM (IC50) | [storage]
Store at -20°C |
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