1. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt
  2. Ras Akt ERK
  3. SS-3091

SS-3091 is a pan-KRas inhibitor active across KRasG12D, KRasG12C, KRasG12V, KRasG12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRasG12 mutations. SS-3091 can be used for the research of KRas-driven cancers.

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SS-3091

SS-3091 Chemical Structure

CAS No. : 2756257-56-2

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Description

SS-3091 is a pan-KRas inhibitor active across KRasG12D, KRasG12C, KRasG12V, KRasG12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRasG12 mutations. SS-3091 can be used for the research of KRas-driven cancers[1].

IC50 & Target[1]

KRas G12C

 

KRas G12D

 

KRas G12V

 

KRas G12S

 

In Vitro

SS-3091 (20-100 μM) directly binds to purified KRASG12D protein, increasing its thermal stability[1].
SS-3091 potently inhibits the proliferation of KRASG12C 4B (IC50 = 27.70 nM), KRASG12C 4A (IC50 = 144.05 nM), KRASG12D 4B (IC50 = 238.15 nM), and KRASG12D 4A (IC50 = 575.00 nM) transformed Ba/F3 cells, with weaker activity against wild-type Ba/F3 cells (IC50 = 2374.00 nM)[1].
SS-3091 potently inhibits proliferation of KRASG12D, KRASG12C, KRASG12V, KRASG12S, and KRASG12A mutant cancer cell lines (IC50 values ranging from 39.23 nM to 1253.60 nM), with weaker or no activity against non-KRAS-driven cancer cell lines[1].
SS-3091 (50-300 nM) dose-dependently suppresses colony formation in PANC1, MIA-PaCa2, SW620, and A549 KRasG12 mutant cancer cell lines[1].
SS-3091 (0-10 μM) dose-dependently inhibits KRas downstream signaling (phosphorylation of S6K, Akt, and ERK) in ASPC1, MIA-PaCa2, SW620, and A549 KRasG12 mutant cancer cell lines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

609.68

Formula

C36H34F3N5O

CAS No.
SMILES

O=C(C1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(C3=CC4=C(C(C)=C3)N=C(NC5=CC=C6C(C(CN(CC6)C)C)=C5)N=C4)=C2

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SS-3091
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HY-178042
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