ACBI3

ACBI3 : panKRAS Degrader (PROTAC)

Structure

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Information

KRAS (Mutant:pan variants)

Degrader (PROTAC)

up to 100 nM

In Vitro Validations

Uniprot ID: P01116

Target Class: Kinase

Target SubClass: Ras Family

Potency: Kd

Potency Value: 6 nM

Potency Assay: SPR for ternary complex with VHL

PDB ID for probe-target interaction (3D structure): 8QU8, 8QVU

Target aliases:

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

DOI Reference: 10.1126/science.adm8684

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): The degradation selectivity of ACBI3 was assessed by whole cell proteomics MS analysis of GP2d cells treated with ACBI3 or the inactive stereoisomer cis-ACBI3 (50 nM). HRAS (log2 fold change -0.0006, -logP 0.001) and NRAS (log2 fold change -0.12, -logP 0.52) levels are not significantly affected.

Potency assay, off target (cells): Proliferation inhibition data was assessed for 240 cancer cell lines for ACBI3

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