An inhibitor of K-RASG12C; decreases the level of active GTP-bound K-RAS by 95% (10 µM); inhibits proliferation preferentially in lung cancer cell lines containing the K-RASG12C mutation

ARS853 – 1 mg

Brand:
Cayman
CAS:
1629268-00-3
Storage:
-20
UN-No:
Non-Hazardous - /

ARS853 is an inhibitor of K-RASG12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells.{30527} ARS853 binds to the inactive GDP-bound state of K-RASG12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RASG12C mutant lung cancer cells. It also decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 µM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.  

 

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Description

An inhibitor of K-RASG12C; decreases the level of active GTP-bound K-RAS by 95% (10 µM); inhibits proliferation preferentially in lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 µM)

Formal name: 1-[3-[4-[2-[[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)phenyl]amino]acetyl]-1-piperazinyl]-1-azetidinyl]-2-propen-1-one

Synonyms: 

Molecular weight: 432.9

CAS: 1629268-00-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|GTPases

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