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Safusidenib

Product Specifications

UNSPSC Description

Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma[1]. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively[2].

Target Antigen

Isocitrate Dehydrogenase (IDH)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/safusidenib.html

Solubility

10 mM in DMSO

Smiles

O=C(N1C2=CC=CC(/C=C/C(O)=O)=C2C(C)=C1)C3=C(C(C)(F)C)ON=C3C4=C(C=C(C=C4Cl)Cl)Cl

Molecular Weight

535.78

References & Citations

[1]Makoto Nakagawa, et al. Selective inhibition of mutant IDH1 by DS-1001b ameliorates aberrant histone modifications and impairs tumor activity in chondrosarcoma. Oncogene. 2019 Oct;38(42):6835-6849.|[2]Yukino Machida, et al. A Potent Blood-Brain Barrier-Permeable Mutant IDH1 Inhibitor Suppresses the Growth of Glioblastoma with IDH1 Mutation in a Patient-Derived Orthotopic Xenograft Model. Mol Cancer Ther. 2020 Feb;19(2):375-383.

Shipping Conditions

Room temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-145594/Safusidenib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-145594/

Clinical Information

Phase 2

CAS Number

1898206-17-1

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