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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.28%
- CAS 番号: 946262-80-2
- 分子式: C20H15ClFN5O2S
- 分子量:443.88
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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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
生物活性
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 % |
化学情報
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CAS 番号 946262-80-2
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性状 Solid
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分子量 443.88
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-159613 関連分類
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