| Identification | Back Directory | [Name]
Benzenemethanesulfonamide, N-[2,3,6-trifluoro-4-[[3-[2-[[(3S,5S)-5-fluoro-3-piperidinyl]amino]-4-pyrimidinyl]-2-pyridinyl]oxy]phenyl]- | [CAS]
2413455-99-7 | [Synonyms]
G-5758
Benzenemethanesulfonamide, N-[2,3,6-trifluoro-4-[[3-[2-[[(3S,5S)-5-fluoro-3-piperidinyl]amino]-4-pyrimidinyl]-2-pyridinyl]oxy]phenyl]- | [Molecular Formula]
C27H24F4N6O3S | [MOL File]
2413455-99-7.mol | [Molecular Weight]
588.58 |
| Chemical Properties | Back Directory | [Boiling point ]
698.7±65.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
7.46±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[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. DOI:10.1021/acs.jmedchem.3c02425 |
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