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bay-293 (c15-1722-032)

BAY-293 (C005B-310241)

Catalog No.
C005B-310241
Manufacturer No.
SML2703-25MG
Manufacturer Name
Sigma-Aldrich
Quantity
25
Unit of Measure
MG

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Biochem/physiol Actions BAY-293 selectively inhibits SOS1-mediated KRAS activation (IC50 = 52 nM: 50 nM wt or G12C hKRAS &: 10 nM SOS1cat) via direct SOS1 binding, blocking SOS1-KRAS interaction (IC50 = 21 nM: 10 nM hSOS1cat &: 5 nM hKRAS

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Biochem/physiol Actions

BAY-293 selectively inhibits SOS1-mediated KRAS activation (IC50 = 52 nM; 50 nM wt or G12C hKRAS & 10 nM SOS1cat) via direct SOS1 binding, blocking SOS1-KRAS interaction (IC50 = 21 nM; 10 nM hSOS1cat & 5 nM hKRAS G12C) without affecting (IC50 >20 μM) CRAF RBD-KRAS interaction, KRAS G12C activation by SOS2, Cdc42 activation by DBS, or EGFR kinase activity. BAY-293 downregulates cellular active RAS (IC50 = 200 nM/Calu-1, 410 nM/HeLa) and downstream ERK phosphorylation (K-562, 150 nM/Calu-1) with good target selectivity as assessed over 358 kinases (<37% inhibition at 1 μM) and a panel of 77 GPCRs, transporters, nuclear receptors and enzymes.

UPC:
41116104
Condition:
New
HazmatClass:
No
MPN:
SML2703-25MG
CAS:
2244904-70-7

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