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Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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SKU | Size | Availability | Price | Qty |
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E648596-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $350.90 | |
E648596-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $580.90 | |
E648596-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,650.90 | |
E648596-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,550.90 |
Specifications & Purity | ≥98% |
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Biochemical and Physiological Mechanisms | EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC In Vitro EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC 50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively. EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549, PC9, H1975, CL68, and CL97 cells Concentration: 0-20 μM Incubation Time: 24 hours, 48 hours, 72 hours Result: Showed inhibitory effects on different cells. Western Blot AnalysisCell Line: A549, PC9, H1975, CL68, and CL97 cells Concentration: 0-0.6 μM Incubation Time: 48 hours Result: Decreased EGFR and c-Met expression. In Vivo EGFR-IN-8 (oral gavage; 50 and 150 mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice H1975 xenograft tumor model Dosage: 50 and 150 mg/kg Administration: Oral gavage; 50 and 150 mg/kg; once daily; 20 days Result: Inhibited H1975 xenograft tumor growth. Form:Solid IC50& Target:EGFR,c-Met |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-[3-chloro-4-[5-[3-[[4-(cyclopropanecarbonylamino)-3-(trifluoromethyl)phenyl]carbamoylamino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]pyridine-3-carboxamide |
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INCHI | InChI=1S/C32H23ClF3N7O4/c33-25-15-22(38-29(45)19-4-2-12-37-16-19)8-10-23(25)27-42-30(47-43-27)18-3-1-5-20(13-18)39-31(46)40-21-9-11-26(24(14-21)32(34,35)36)41-28(44)17-6-7-17/h1-5,8-17H,6-7H2,(H,38,45)(H,41,44)(H2,39,40,46) |
InChi Key | IIUNSVLRVWGJRM-UHFFFAOYSA-N |
Canonical SMILES | C1CC1C(=O)NC2=C(C=C(C=C2)NC(=O)NC3=CC=CC(=C3)C4=NC(=NO4)C5=C(C=C(C=C5)NC(=O)C6=CN=CC=C6)Cl)C(F)(F)F |
Isomeric SMILES | C1CC1C(=O)NC2=C(C=C(C=C2)NC(=O)NC3=CC=CC(=C3)C4=NC(=NO4)C5=C(C=C(C=C5)NC(=O)C6=CN=CC=C6)Cl)C(F)(F)F |
PubChem CID | 139035057 |
Molecular Weight | 662.02 |
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Solubility | DMSO : 8.33 mg/mL (12.58 mM; Need ultrasonic) |
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