K-Ras(G12C) inhibitor 9

Bezeichnung:K-Ras(G12C) inhibitor 9

CAS-Nr1469337-91-4

Englisch Name:K-Ras(G12C) inhibitor 9

CBNumberCB32722367

SummenformelC16H21ClIN3O4S

Molgewicht513.78

MOL-Datei1469337-91-4.mol

K-Ras(G12C) inhibitor 9 physikalisch-chemischer Eigenschaften

Siedepunkt	656.3±65.0 °C(Predicted)
Dichte	1.68±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	Soluble in DMSO
Aggregatzustand	crystalline solid
pka	9.68±0.20(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

K-Ras(G12C) inhibitor 9 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
K-Ras(G12C) inhibitor 9 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant that causes 100% modification of the protein when used at 10 μM for 24 hours in vitro. K-Ras is a small GTPase that cycles between a GTP-bound active state and a GDP-bound inactive state to turn on downstream Raf kinases to drive cell growth. A G12C mutation in K-Ras blocks GTP hydrolysis, activates K-Ras, and promotes carcinogenesis. Similar K-Ras(G12C) inhibitors significantly reduce GTP affinity relative to GDP, decrease Raf binding, and lower cell viability while increasing apoptosis.
Verwenden
N-[1-[2-[(4-Chloro-5-iodo-2-methoxyphenyl)amino]acetyl]-4-piperidinyl]ethenesulfonamide is an allosteric inhibitor of tumor-promoting K-Ras(G12c).
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].
target
k-ras(g12c)
Einzelnachweise
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.

K-Ras(G12C) inhibitor 9 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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