|
| | K-Ras(G12C) inhibitor 6 Basic information |
| Product Name: | K-Ras(G12C) inhibitor 6 | | Synonyms: | K-Ras(G12C) inhibitor 6;Butanamide, N-[1-[2-(2,4-dichlorophenoxy)acetyl]-4-piperidinyl]-4-mercapto-;K-Ras(G12C) inhibitor 6 USP/EP/BP;N-?[1-?[2-?(2,?4-Dichlorophenoxy)?acetyl]?-?4-?piperidinyl]?-?4-?mercapto-butanamide;N-[1-[2-(2,4-dichlorophenoxy)acetyl]piperidin-4-yl]-4-sulfanylbutanamide;CS-2013;MDK30165;Ras,inhibit,Inhibitor,K-Ras(G12C) inhibitor 6,K Ras(G12C) Inhibitor 6,KRas(G12C) Inhibitor 6,K-Ras(G-12C) Inhibitor 6 | | CAS: | 2060530-16-5 | | MF: | C17H22Cl2N2O3S | | MW: | 405.34 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 2060530-16-5.mol |  |
| | 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 Preparation Products And Raw materials |
|
