PELP1-IN-1
Based on 1 Customer Validation
PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER+ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer.
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- Purity: 99.28%
- CAS No.: 946262-80-2
- 화학식: C20H15ClFN5O2S
- 분자량:443.88
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Anti-Cancer Compound Library
HY-L025
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Anti-Breast Cancer Compound Library
HY-L074
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Nuclear Receptor Compound Library
HY-L126
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Membrane Receptor-targeted Compound Library
HY-L150
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Cell Death Library
HY-L162
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Anti-Drug-Resistant Compound Library
HY-L169
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
PELP1[1]
PELP1-IN-1 (SM1) (10 μM; 12-48 h) inhibits migration and invasion of ZR75, MCF7 and MT-ER+ breast cancer cells, reduces soft agar colony formation, promotes apoptosis (Annexin V staining, increased caspase 3/7 activity) and induces S-phase cell cycle arrest[1].
PELP1-IN-1 (10 μM; 48 h) downregulates the expression of estrogen response- and cell cycle-related genes, upregulates genes involved in the apoptosis and p53 pathways, and inhibits ER-PELP1 downstream signaling in ZR75 and MCF7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ZR75, MCF7, MCF7(Y537S), MCF7(D538G), ZR75(Y537S), ZR75(D538G)
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Concentration:10 μM
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Incubation Time:24-48 h
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Result:Induced apoptosis in both WT-ER+ and MT-ER+ breast cancer cells, as indicated by increased Annexin V-positive cells and enhanced caspase 3/7 enzymatic activity.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | CL | Vd | Cmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[2] | 1 mg/kg | i.v. | 970.4 ng·h/mL | 986.7 ng·h/mL | 1.6 h | 1.8 h | 1.3 h | 0.1 h | 1.2 L/h/kg | 2.1 L/kg | 583.4 ng/mL | / |
| Mice[2] | 1 mg/kg | i.v. | 970.4 ng·h/mL | 986.7 ng·h/mL | 1.6 h | 1.8 h | 1.3 h | 0.1 h | 1.2 L/h/kg | 2.1 L/kg | 583.4 ng/mL | / |
| Mice[2] | 1 mg/kg | i.v. | 970.4 ng·h/mL | 986.7 ng·h/mL | 1.6 h | 1.8 h | 1.3 h | 0.1 h | 1.2 L/h/kg | 2.1 L/kg | 583.4 ng/mL | / |
| Mice[2] | 2 mg/kg | p.o. | 1261.6 ng·h/mL | 1419.6 ng·h/mL | 2.1 h | 3.2 h | 2.5 h | 0.8 h | 1.5 L/h/kg | 4.9 L/kg | 614.8 ng/mL | 65.0 % |
| Mice[2] | 2 mg/kg | p.o. | 1261.6 ng·h/mL | 1419.6 ng·h/mL | 2.1 h | 3.2 h | 2.5 h | 0.8 h | 1.5 L/h/kg | 4.9 L/kg | 614.8 ng/mL | 65.0 % |
| Mice[2] | 2 mg/kg | p.o. | 1261.6 ng·h/mL | 1419.6 ng·h/mL | 2.1 h | 3.2 h | 2.5 h | 0.8 h | 1.5 L/h/kg | 4.9 L/kg | 614.8 ng/mL | 65.0 % |
| Mice[2] | 4 mg/kg | p.o. | 3023.6 ng·h/mL | 3050.8 ng·h/mL | 1.6 h | 1.7 h | 1.2 h | 0.8 h | 1.4 L/h/kg | 2.4 L/kg | 1716.6 ng/mL | 77.9 % |
| Mice[2] | 4 mg/kg | p.o. | 3023.6 ng·h/mL | 3050.8 ng·h/mL | 1.6 h | 1.7 h | 1.2 h | 0.8 h | 1.4 L/h/kg | 2.4 L/kg | 1716.6 ng/mL | 77.9 % |
| Mice[2] | 4 mg/kg | p.o. | 3023.6 ng·h/mL | 3050.8 ng·h/mL | 1.6 h | 1.7 h | 1.2 h | 0.8 h | 1.4 L/h/kg | 2.4 L/kg | 1716.6 ng/mL | 77.9 % |
| Mice[2] | 8 mg/kg | p.o. | 6149.6 ng·h/mL | 6208.9 ng·h/mL | 1.6 h | 1.7 h | 1.1 h | 0.8 h | 1.3 L/h/kg | 2.0 L/kg | 3045.6 ng/mL | 79.2 % |
| Mice[2] | 8 mg/kg | p.o. | 6149.6 ng·h/mL | 6208.9 ng·h/mL | 1.6 h | 1.7 h | 1.1 h | 0.8 h | 1.3 L/h/kg | 2.0 L/kg | 3045.6 ng/mL | 79.2 % |
| Mice[2] | 8 mg/kg | p.o. | 6149.6 ng·h/mL | 6208.9 ng·h/mL | 1.6 h | 1.7 h | 1.1 h | 0.8 h | 1.3 L/h/kg | 2.0 L/kg | 3045.6 ng/mL | 79.2 % |
Chemical Information
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CAS No. 946262-80-2
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Appearance Solid
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분자량 443.88
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화학식 C20H15ClFN5O2S
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Color White to off-white
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SMILES
O=C1C2=C(N(C3=CC=C(Cl)C=C3)N=C2)N=C(SCC(NCC4=CC=C(F)C=C4)=O)N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 4.57 mg/mL (10.30 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2529 mL | 11.2643 mL | 22.5286 mL | 56.3215 mL |
| 5 mM | 0.4506 mL | 2.2529 mL | 4.5057 mL | 11.2643 mL | |
| 10 mM | 0.2253 mL | 1.1264 mL | 2.2529 mL | 5.6322 mL |
PELP1-IN-1 Related Classifications
HY-159613 Related Classifications
Powered by Bioz
- PELP1-IN-1
- 946262-80-2
- Apoptosis
- Estrogen Receptor/ERR
- mammary epithelial cells
- ovarian epithelial cells
- wild-type ER+ breast cancer
- therapy-resistant ER+ breast cancer
- endometrial epithelial cells
- PELP1
- mutant ER+ breast cancer
- proteasome pathway
- estrogen receptor alpha-positive breast cancers
- Inhibitor
- inhibitor
- inhibit