| Identification | Back Directory | [Name]
Benzamide, 4-[[3-(2-hydroxyethoxy)-4-nitrobenzoyl]amino]-N-[4-[[(trans-4-methylcyclohexyl)amino]carbonyl]-2-(2-methylpropoxy)phenyl]-3-(2-methylpropoxy)- | [CAS]
2440087-54-5 | [Synonyms]
Benzamide, 4-[[3-(2-hydroxyethoxy)-4-nitrobenzoyl]amino]-N-[4-[[(trans-4-methylcyclohexyl)amino]carbonyl]-2-(2-methylpropoxy)phenyl]-3-(2-methylpropoxy)- | [Molecular Formula]
C38H48N4O9 | [MOL File]
2440087-54-5.mol | [Molecular Weight]
704.81 |
| Chemical Properties | Back Directory | [Boiling point ]
774.0±60.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [solubility ]
DMF: 5 mg/ml; DMSO: Slightly soluble | [form ]
A solid | [pka]
10.65±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
ERX-41 is an inducer of endoplasmic reticulum (ER) stress.1 It increases the thermal stability of lysosomal acid lipase when used at a concentration of 10 μM in the cellular thermal shift assay (CETSA) but does not inhibit lysosomal acid lipase enzymatic activity at 30 μM. ERX-41 (1 μM) increases ER tubule width, eukaryotic translation initiation factor 2α kinase 3 (EIF2AK3/PERK) and inositol-requiring enzyme 1α (IRE1α) phosphorylation, and splicing of the gene encoding X-box binding protein 1 (XBP1) in SUM149 triple-negative breast cancer (TNBC) cells. It reduces tumor volume and weight in several patient-derived xenograft (PDX) mouse models of TNBC when administered at a dose of 10 mg/kg. | [Uses]
ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors[1]. | [in vivo]
ERX-41 (10 mg/kg; p.o. or i.p.; single dose) is detectable within 1.5?h in established s.c. MDA-MB-231 xenografts after either PO or i.p. administration[1].
ERX-41 (10 mg/kg; p.o.; single dose) significantly inhibits the progression without changing body weight in mouse model with MDA-MB-231 xenografts[1].
ERX-41 (10 mg/kg; p.o. or i.p.; single dose) significantly inhibits the progression in mouse model with MDA-MB-231 s.c. xenografts[1].
| Animal Model: | Mouse models with D2A1 xenografts and MDA-MB-231 xenografts (s.c.), respectively[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; once daily for 25 days | | Result: | Reduced tumor growth against MDA-MB-231 xenograft without affecting body weight. And enhanced p-PERK and p-eIF2-α staining within 24?h.
Significantly reduced the growth of D2A1 xenografts in syngeneic mice without affecting body weight. |
| [References]
1. Liu, X., Viswanadhapalli, S., Kumar, S., et al. Targeting LIPA independent of its lipase activity is a therapeutic strategy in solid tumors via induction of endoplasmic reticulum stress Nat. Cancer 3(7),866-884(2022). |
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