2761170-84-5
Chemical Structure
ABS-752
- CAS No.: 2761170-84-5
- Formula:C14H14FN3O3
- Molecular Weight:291.28
IUPAC Name: 3-(5-(aminomethyl)-6-fluoro-1-oxoisoindolin-2-yl)piperidine-2,6-dione
InChIKey: VHUZYSKPEQGBJP-UHFFFAOYSA-N
SMILES: O=C(C(N(CC1=C2C=C(F)C(CN)=C1)C2=O)CC3)NC3=O
Biological Activity: ABS-752 is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 shows no cytotoxicity in primary human hepatocytes. ABS-752 can be used in the research of hepatocellular carcinoma[1].
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ABS-752 | ABS-752 is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 shows no cytotoxicity in primary human hepatocytes. ABS-752 can be used in the research of hepatocellular carcinoma. | |||||||||||||||||||||
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