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G-5758

Product Specifications

UNSPSC Description

G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown[1].

Target Antigen

IRE1; Liposome

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage;Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

cancer

Assay Protocol

https://www.medchemexpress.com/g-5758.html

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC1=C(F)C(NS(CC2=CC=CC=C2)(=O)=O)=C(F)C=C1OC3=C(C=CC=N3)C4=CC=NC(N[C@H]5C[C@H](F)CNC5)=N4

Molecular Weight

588.58

References & Citations

[1]Braun MG, et al. Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model. J Med Chem. 2024 Jun 13;67(11):8708-8729.

Shipping Conditions

Room Temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-161672/G-5758-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-161672/G-5758-SDS-MedChemExpress.pdf

Clinical Information

No Development Reported

CAS Number

2413455-99-7

Available Sizes

Curated Selection

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