product name K-Ras(G12C) inhibitor 9
Description: K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). Ras proteins belong to the large family of GTPase enzymes which are essential to transduce extracellular signals into diverse cellular responses including proliferation, differentiation, and apoptosis. About 30% of all human cancers contain activating Ras mutations, making them one of the most common known genetic molecular drivers of cancer. Therefore, K-Ras signaling have potential therapeutic advantages in cancer.
References: Nature. 2013 Nov 28;503(7477):548-51.
513.78
Formula
C16H21ClIN3O4S
CAS No.
1469337-91-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (103.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: K-Ras(G12C) inhibitor 9 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 9 belongs to a series of small molecules, which irreversibly compete with GTP and GDP for binding to a common oncogenic K-Ras(G12C) mutant and blocked the association of B-Raf and C-Raf with K-Ras(G12C). K-Ras(G12C) inhibitor 9 (10 μM) decreased viability and increased apoptosis of G12C mutations-containing lung cancer cell lines (H1792, Calu-1, H358, and H23) |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Nature. 2013 Nov 28;503(7477):548-51. |
