| Identification | Back Directory | [Name]
K-Ras(G12C) inhibitor 9 | [CAS]
1469337-91-4 | [Synonyms]
K-RAS inhibitor 9
K-Ras(G12C) inhibitor 9
K-Ras(G12C) inhibitor 9 USP/EP/BP
K RAS INHIBITOR-9; KRAS INHIBITOR 9
N-[1-[2-[(4-chloro-5-iodo-2-methoxyphenyl)amino]acetyl]-4-piperidinyl]-ethenesulfonamide
Ethenesulfonamide, N-[1-[2-[(4-chloro-5-iodo-2-methoxyphenyl)amino]acetyl]-4-piperidinyl]- | [Molecular Formula]
C16H21ClIN3O4S | [MDL Number]
MFCD28143916 | [MOL File]
1469337-91-4.mol | [Molecular Weight]
513.78 |
| Chemical Properties | Back Directory | [Boiling point ]
656.3±65.0 °C(Predicted) | [density ]
1.68±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
9.68±0.20(Predicted) |
| Hazard Information | Back Directory | [Description]
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.1 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.2,3 Similar K-Ras(G12C) inhibitors significantly reduce GTP affinity relative to GDP, decrease Raf binding, and lower cell viability while increasing apoptosis.1 | [Uses]
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) | [storage]
Store at -20°C | [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. |
|
| Company Name: |
D&C Chemicals
|
| Tel: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0.htm |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|