| Identification | Back Directory | [Name]
K-Ras(G12C) inhibitor 6 | [CAS]
2060530-16-5 | [Synonyms]
CS-2013
MDK30165
K-Ras(G12C) inhibitor 6
K-Ras(G12C) inhibitor 6 USP/EP/BP
N-[1-[2-(2,4-dichlorophenoxy)acetyl]piperidin-4-yl]-4-sulfanylbutanamide
Butanamide, N-[1-[2-(2,4-dichlorophenoxy)acetyl]-4-piperidinyl]-4-mercapto-
N-?[1-?[2-?(2,?4-Dichlorophenoxy)?acetyl]?-?4-?piperidinyl]?-?4-?mercapto-butanamide | [Molecular Formula]
C17H22Cl2N2O3S | [MDL Number]
MFCD28099807 | [MOL File]
2060530-16-5.mol | [Molecular Weight]
405.34 |
| Chemical Properties | Back Directory | [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) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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]. | [IC 50]
K-Ras(G12C) | [storage]
Store at -20°C | [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. |
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Twochem Co.Ltd.
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021-58111628 15800915896 |
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cn.twochem.com |
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