product name K-Ras(G12C) inhibitor 12
Description: K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). K-Ras(G12C) exhibited a slight preference for GTP. However, K-Ras(G12C) inhibitor 12 significantly reduced the affinity for GTP and led to the modification of K-Ras(G12C). Also, K-Ras(G12C) inhibitor 12 inhibited SOS-catalysed nucleotide exchange. In H1792 and H358 K-Ras(G12C)-mutant lung cancer cell lines, K-Ras(G12C) inhibitor 12 reduced the association of C-Raf and B-Raf with Ras.
References: Nature. 2013 Nov 28;503(7477):548-51.
449.67
Formula
C15H17ClIN3O3
CAS No.
1469337-95-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 27 mg/mL (60.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: K-Ras(G12C) inhibitor 12 belongs to a series of small molecules, which irreversibly bind to a common oncogenic mutant K-Ras(G12C) and blocks K-Ras(G12C) interactions. Some of them decrease viability and increase apoptosis of G12C-containing cancer cell lines. Kinase Assay: Cell Assay: K-Ras(G12C) inhibitor 12 is a highly effective Ras inhibitor and its EC50 value in H1792 cells is 0.32 μM.It selectively binds to an oncogenic mutant K-Ras(G12C) in a irreversible manner without affecting the activity of wild-type Ras. After treatment with K-Ras(G12C) inhibitor 12, K-Ras(G12C)-mutant cells exhibit decreased viability and increased apoptosis comparing to cells lacking this mutation. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nature. 2013 Nov 28;503(7477):548-51. |
