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G12Si-5

Chemical Structure : G12Si-5

CAS No.:

G12Si-5

Catalog No.: PC-49153Not For Human Use, Lab Use Only.

G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.
G12Si-5 inhibits Ras signaling in A549 cells with IC50 of 3 uM, does not perturb the signaling in A375 cells (wild-type KRAS) or SW1990 cells (homozygous KRAS p.G12D).
G12Si-5 dose-dependently reduces phospho-ERK levels in Ba/F3:K-Ras(G12S) cells, also inhibits the growth of KMS20, a patient-derived myeloma cell line with a homozygous KRAS p.G12S mutation, with IC50 of 7.5 uM.

Physicochemical Properties

M.Wt 574.053
Formula C31H29ClFN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

1. Ziyang Zhang, et al. Nat Chem Biol. 2022 Jul 21. doi: 10.1038/s41589-022-01065-9.

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