Toggle Nav

K-Ras(G12C) inhibitor 6

In stock
Catalog No.
B3694
K-Ras (G12C) inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$130.00
In stock
10mg
$200.00
In stock
25mg
$420.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

K-Ras (G12C) inhibitor 6 is an allosterical inhibitor of oncogenic mutation K-Ras G12C [1].

K-Ras (G12C) inhibitor 6 is a cysteine-reactive small molecule. It irreversibly binds to the G12C mutantion of GTPase K-Ras but not the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras. Since the mutation of K-Ras is quite common in human cancers, the inhibitor of K-Ras G12C should exert suppression activities in tumor cells. It has been reported that, some of the K-Ras G12C inhibitors are indeed effective to decrease cell viability and increase apoptosis in lung cancer cell lines [1].

References:
[1] Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt405.34
Cas No.2060530-16-5
FormulaC17H22Cl2N2O3S
Solubility≥20.25mg/mL in DMSO
SDFDownload SDF
Canonical SMILESC1CN(CCC1NC(=O)CCCS)C(=O)COC2=C(C=C(C=C2)Cl)Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
Targets K-Ras(G12C)          
IC50            

Quality Control

Chemical structure

K-Ras(G12C) inhibitor 6