Anticancer agent 98
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min.
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- No. CAS: 2857070-72-3
- Fòrmula: C17H19N5O2
- Peso molecular:325.37
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Anticancer agent 98 inhibits cancer proliferation among melanoma, breast cancer, and pancreatic cancer with IC50s ranging from 0.6-3 nM[1].
Anticancer agent 98 (300 nM, 1 μM, or 3 μM; 2 h) increases β-tubulin adduct in PC-3 cells dose-dependently[1].
Anticancer agent 98 (3.125, 6.25, 12.5, 25, and 50 μM) has high-binding affinity to tubulin proteins with Kd value of 16.9 μM by SPR spectroscopy assay[1].
Anticancer agent 98 (10 μM, 50 μM; 0-60 min) strongly inhibits tubulin polymerization during 60 min[1].
Anticancer agent 98 (100 nM; 4 h) has antiproliferative and anti-angiogenesis effect on COS-7 cells in vitro[1].
In Vitro Metabolic Stability[1]
| human microsomes | mouse microsomes | ||
| t1/2 (min) | CLint (μL/min/mg) | t1/2 (min) | CLint (μL/min/mg) |
| >300 | <2.31 | >300 | <2.31 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis in NSG Mice[1]
| Route | Dose (mg/kg) | Cmax (ng/mL) | tmax (min) | AUC (ng·min/mL) | t1/2 (min) | F (%) |
| i.v. | 4 | 1247 | 5.0 | 173,476 | 238 | / |
| p.o. | 10 | 78.3 | 10.0 | 8161 | 358 | 2.02 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC3/TxR xenograft model in NSG mouse[1]
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Dosage:2.5 mg/kg
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Administration:IV; twice weekly for 2 weeks
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Result:Inhibited the tumor growth in volume by approximately 85.6%. And inhibited angiogenesis by 44% related to control group.
Overcame taxane resistance at a low, safe, but potent dose in vivo.
Chemical Information
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No. CAS 2857070-72-3
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Peso molecular 325.37
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Fòrmula C17H19N5O2
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SMILES
O=C1NC2=CC(OC)=CC=C2N(C1)C3=NC(NC)=NC4=C3CCC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anticancer agent 98 Related Classifications
HY-149920 Related Classifications
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