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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C49H48N8O6
- 분자량:844.96
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
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.
-
Cell Line:SHEP MYCN-ER cells
-
Concentration:0.1, 1, 10, 50, 100 µM
-
Incubation Time:0.5, 1, 2, 4, 6 h
-
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.
-
Animal Model:T409 xenografts model[1].
-
Dosage:30 mg/kg
-
Administration:Intraperitoneal injection; once daily for 15 days
-
Result:Inhibited the growth of NUDT1-related tumor.
-
Animal Model:Male C57BL/6 mice[1].
-
Dosage:50 mg/kg, 30 mg/kg
-
Administration:Intravenous/Intraperitoneal/Oral; single dose
-
Result:Exhibited an oral bioavailability of 14.2%, nominating it as a promising lead for further optimization
Chemical Information
-
분자량 844.96
-
화학식 C49H48N8O6
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LC-1-40 Related Classifications
HY-158062 Related Classifications
Powered by Bioz