LC-1-40
LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
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- Fòrmula: C49H48N8O6
- Peso molecular:844.96
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
DC50: 0.97 nM (NUDT1)[1].
LC-1-40 (0.1, 1, 10, 50, 100 µM; 0.5, 1, 2, 4, 6 h) induces a dose- and time-dependent NUDT1 degradation in SHEP MYCN-ER cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SHEP MYCN-ER cells
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Concentration:0.1, 1, 10, 50, 100 µM
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Incubation Time:0.5, 1, 2, 4, 6 h
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Result:Induced NUDT1 degradation in a dose- and time-dependent manner.
| IV (5 mg/kg) | IP (30 mg/kg) | PO (30 mg/kg) | |
| T1/2 (h) | 6.34 | 42.7 | 7.13 |
| Tmax (h) | 0.08 | 3.33 | 3.33 |
| Cmax (ng/mL) | 4373 | 3080 | 1923 |
| AUCInf (h*ng/mL) | 32571 | 59799 | 25063 |
| CL (mL/min/kg) | 2.57 | - | - |
| Vss (mL/kg) | 1.2 | - | - |
| F (%) | - | 32.7 | 14.2 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:T409 xenografts model[1].
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection; once daily for 15 days
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Result:Inhibited the growth of NUDT1-related tumor.
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Animal Model:Male C57BL/6 mice[1].
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Dosage:50 mg/kg, 30 mg/kg
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Administration:Intravenous/Intraperitoneal/Oral; single dose
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Result:Exhibited an oral bioavailability of 14.2%, nominating it as a promising lead for further optimization
Chemical Information
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Peso molecular 844.96
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Fòrmula C49H48N8O6
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SMILES
O=C1CCC(C(N1)=O)N2C(C3=C(C2=O)C=C(C=C3)N4CCN(CC4)CC5CCN(CC5)C(C6=CC=C(C=C6)C7=CC=C8N=CC(C(NC9CC9)=O)=C(C8=C7)NC%10=CC=CC=C%10)=O)=O
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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)
LC-1-40 Related Classifications
HY-158062 Related Classifications
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