ARS-1620

Covalent Inhibitor of KRAS (Mutant:G12C)

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe ARS-1620 is in the process of SERP review.

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Information

KRAS (Mutant:G12C)

Covalent Inhibitor

0.3 - 3.0 uM

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Probe Availability:

In Vitro Validations

Uniprot ID: P01116

Target Class: GTPase

Target SubClass: GTPase

Potency: kobs/[I]

Potency Value: 1,100 ± 200 M−1 s−1

Potency Assay: kobs/[I] determined by Biochemical Binding Assay

PDB ID for probe-target interaction (3D structure): 5V9U

Structure-activity relationship: yes

Target aliases:

GTPase KRas, RASK2, KRAS2, KRAS, RASK_HUMAN, c-Ki- ...

DOI Reference: 10.1016/j.cell.2018.01.006

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

Proteome and Transcriptome Profiling the Functional Selectivity of ARS-1620 for KRASG12C and Associated Gene Transcription Signatures

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Less potent than later KRAS(G12C) inhibitors

(last updated: 15 Feb 2024 )