| Identification | Back Directory | [Name]
RVX297 | [CAS]
1044871-04-6 | [Synonyms]
RVX297
2-(3,5-Dimethyl-4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one
4(3H)-Quinazolinone, 2-[3,5-dimethyl-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-5,7-dimethoxy-
autoimmunity,RVX 297,proinflammatory,Epigenetic Reader Domain,RVX-297,immune,inhibit,mediator,inflammatory,Inhibitor,selectivity,acute,cell,arthritis | [Molecular Formula]
C24H29N3O4 | [MDL Number]
MFCD32710231 | [MOL File]
1044871-04-6.mol | [Molecular Weight]
423.5 |
| Chemical Properties | Back Directory | [Boiling point ]
612.6±65.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (118.06 mM; Need ultrasonic) | [form ]
Solid | [pka]
9.54±0.20(Predicted) | [color ]
White to light brown |
| Hazard Information | Back Directory | [Uses]
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2]. | [in vivo]
RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model[1].
RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model[1].
RVX-297 suppresses cytokine production in LPS-treated mice[1]. | Animal Model: | Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis)[1] | | Dosage: | 25, 50, and 75 mg/kg | | Administration: | P.o.; per day for 6 days | | Result: | Prevented swelling and inflammation of the ankle and knee joints.
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| [IC 50]
BRD2 (BD1): 3.76 μM (IC50); BRD2 (BD2): 0.08 μM (IC50); BRD3 (BD1): 2.34 μM (IC50); BRD3 (BD2): 0.05 μM (IC50); BRD4 (BD1): 1.16 μM (IC50); BRD4 (BD2): 0.02 μM (IC50); BRDT (BD1): 2.69 μM (IC50) | [References]
[1] Jahagirdar R, et al. RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease. Mol Pharmacol. 2017;92(6):694-706. DOI:10.1124/mol.117.110379
[2] Kharenko OA, et al. RVX-297- a novel BD2 selective inhibitor of BET bromodomains. Biochem Biophys Res Commun. 2016;477(1):62-67. DOI:10.1016/j.bbrc.2016.06.021 |
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