KRASG12C IN-19
KRASG12C IN-19 is a selective and orally active KRASG12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRASG12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM) . KRASG12C IN 19 has no significant inhibitory activity against KRASG12V and KRASG12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRASG12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRASG12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer[1].
Product Specifications
CAS Number
[2915282-32-3]
UNSPSC
12352005
Target
ERK; Reactive Oxygen Species (ROS)
Related Pathways
Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; NF-κB; Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
C=CC(N1C[C@@H](N(C[C@H]1C)C2=NC(N(C3=C2C=C(C(C4=CC=CC=C4F)=N3)C#N)C5=C(N=CN=C5C6CC6)C7CC7)=O)C)=O
Molecular Formula
C33H31FN8O2
Molecular Weight
590.65
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ERK
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