K-Ras(G12C) inhibitor 6 Chemical Properties

Boiling point:

643.4±55.0 °C(Predicted)

Density 

1.34±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; insoluble in EtOH; ≥20.25 mg/mL in DMSO

form 

solid

pka

10.21±0.10(Predicted)

K-Ras(G12C) inhibitor 6 Usage And Synthesis

Uses

N-?[1-?[2-?(2,?4-Dichlorophenoxy)?acetyl]?-?4-?piperidinyl]?-?4-?mercapto-butanamide is an irreversible and allosteric inhibitor of the K-Ras(G12C) mutant. This compound has potential therapeutic application for diseases related to Ras signaling.

Biological Activity

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.

K-Ras(G12C) inhibitor 6(2060530-16-5)Related Product Information

• lysyllysine
• Creatine Phosphokinase
• K-Ras inhibitor
• Paclitaxel
• K-Ras(G12C) inhibitor 9
• LB 42708
• Erlotinib hydrochloride
• 1-(4-(2-((4-chloro-2-hydroxy-5-iodophenyl)aMino)acetyl)piperazin-1-yl)prop-2-en-1-one