K-Ras(G12C) inhibitor 6
- CAS NO.:2060530-16-5
- Empirical Formula: C17H22Cl2N2O3S
- Molecular Weight: 405.34
- MDL number: MFCD28099807
- Update Date: 2023-05-21 10:59:17
What is K-Ras(G12C) inhibitor 6?
The Uses of K-Ras(G12C) inhibitor 6
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.
Properties of K-Ras(G12C) inhibitor 6
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) |
Safety information for K-Ras(G12C) inhibitor 6
Computed Descriptors for K-Ras(G12C) inhibitor 6
New Products
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