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K-Ras(G12C) inhibitor 9

In stock
Catalog No.
B6002
allosteric inhibitor of oncogenic K-Ras(G12C)
Grouped product items
SizePriceStock Qty
5mg
$190.00
In stock
10mg
$336.00
In stock
25mg
$526.00
In stock

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Background

Target: K-Ras(G12C)

IC50: N/A

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C) [1]. 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 [2]. Therefore, K-Ras signaling have potential therapeutic advantages in cancer. K-Ras(G12C) is present in roughly 10–20% of Ras-driven cancers and in an estimated 50% of Ras-mutated lung adenocarcinomas [3].

In vitro: 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) [1].

In vivo: N/A

References:
1.  Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013;503(7477):548-51.
2.  Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, et al. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014;111(24):8895-900.
3.  Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014;53(1):199-204.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt513.78
Cas No.1469337-91-4
FormulaC16H21ClIN3O4S
SolubilitySoluble in DMSO
Chemical NameN-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide
SDFDownload SDF
Canonical SMILESC=CS(NC1CCN(C(CNC2=C(OC)C=C(Cl)C(I)=C2)=O)CC1)(=O)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

K-Ras(G12C) inhibitor 9