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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1 -dependent apoptosis . cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models
In Vitro
cRIPGBM chloride (0.25 μM; 0-24 h) time-dependently activates caspase 1, caspase 9, and caspase 7, as well as PARP cleavage, in CBM-1 GBM CSCs. cRIPGBM chloride (0.125 μM, 0.25 μM; 24 h) induces cell apoptosis mediated by caspase 1 in CBM-1 GBM CSCs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: GBM-1 GBM CSCs Concentration: 50 nM, 100 nM, 125 nM, 250 nM, and 500 nM Incubation Time: 3 h, 6 h, 12 h, and 24 h Result: Had the ability to regulate RIPK2 to act as a prosurvival or proapoptotic molecule. Significantly reduced RIPK2 binding to cIAP2 in a dose-dependent manner.
In Vivo
cRIPGBM chloride (50 mg/kg; p.o.; twice daily for 5 weeks) inhibits tumor growth in patient-derived GBM CSC intracranial xenograft mouse models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Orthotopic intracranial xenograft model in mouse Dosage: 50 mg/kg Administration: PO; twice daily, 8 h apart, starting at day 7 postinjection; last for 5 weeks Result: Monitored by Fluorescence Tomography System. Decreased the tumor signal, as well as tumor size.
Form:Solid
IC50& Target:Caspase-1 RIPK2
| Sonrisas canónicas | CC1=[N+](C2=C(N1CC3=CC=C(C=C3)F)C(=O)C4=CC=CC=C4C2=O)CC5=CC=CC=C5.[Cl-] |
|---|---|
| IUPAC Name | 3-benzyl-1-[(4-fluorophenyl)methyl]-2-methylbenzo[f]benzimidazol-3-ium-4,9-dione;chloride |
| InChIKey | IHNGETPFBJHWFE-UHFFFAOYSA-M |
| INCHI | 1S/C26H20FN2O2.ClH/c1-17-28(15-18-7-3-2-4-8-18)23-24(29(17)16-19-11-13-20(27)14-12-19)26(31)22-10-6-5-9-21(22)25(23)30;/h2-14H,15-16H2,1H3;1H/q+1;/p-1 |
| PubChem CID | 156024495 |
| Peso molecular | 446.90 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubilidad | DMSO : 25 mg/mL (55.94 mM; ultrasonic and warming and heat to 60°C) |
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