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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