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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

[1]Fang Yang, et al.Design, synthesis and evaluation of 1,2-dihydropyrido[2,3-d]pyrimidine-6‑carbonitrile derivatives as novel covalent inhibitors for the treatment of KRASG12C-mutant NSCLC, Bioorganic Chemistry

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

ERK

Curated Selection

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