1. GPCR/G Protein
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  3. G12Si-5 formic

G12Si-5 formic 

Cat. No.: HY-150054A
Handling Instructions

G12Si-5 formic is a covalent inhibitor of the G12S mutant of K-Ras (Ki: 26 μM). G12Si-5 formic binds with the S-IIP domain and suppresses oncogenic signaling. G12Si-5 formic reduces phospho-ERK level in KRAS G12S mutated cells.

For research use only. We do not sell to patients.

G12Si-5 formic Chemical Structure

G12Si-5 formic Chemical Structure

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Description

G12Si-5 formic is a covalent inhibitor of the G12S mutant of K-Ras (Ki: 26 μM). G12Si-5 formic binds with the S-IIP domain and suppresses oncogenic signaling. G12Si-5 formic reduces phospho-ERK level in KRAS G12S mutated cells[1].

IC50 & Target[1]

KRas G12S

26 μM (Ki)

In Vitro

G12Si-5 (10 μM, 2 h) formic leads to nearly complete loss of Ras•GTP and concomitant inhibition of phospho-ERK in A549 cells[1].
G12Si-5 (10 μM, 2 h) formic leads to a reduction in the phospho-ERK level and gel-mobility shift of the K-Ras protein in cell lines with confirmed KRAS p.G12S mutations (A549, KMS20)[1].
G12Si-5 (100 μM, 72 h) formic inhibits the growth of the K-Ras(G12S)-transduced Ba/F3 cells with an IC50 of 2.4 μM[1].

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

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0, 0.37, 1.1, 3.3, 10, 30 μM
Incubation Time: 2 h
Result: Dose-dependently decreased Ras (G12S) and p-ERK expression.
Molecular Weight

620.07

Formula

C32H31ClFN5O5

SMILES

ClC1=CC=CC2=CC=CC(C3=C(F)C4=C(C(N5CC[[email protected]]6C(O[[email protected]]6C5)=O)=NC(OCC78CCCN7CCC8)=N4)C=N3)=C12.OC=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Product Name:
G12Si-5 formic
Cat. No.:
HY-150054A
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