SP27
Based on 1 Customer Validation
SP27 is a PROTAC PLK4 degrader with an IC50 of 8.4 nM and a DC50 of 19.5 nM against PLK4. SP27 induces PLK4 degradation via the CRBN-dependent ubiquitin-proteasome pathway, inhibits PLK4 downstream signal transduction, and suppresses the growth of TRIM37-amplified breast cancer cells. SP27 is applicable for breast cancer-related research.
(Pink: PLK4 ligand (HY-128493); Blue: Cereblon ligand (HY-14658); Black: linker).
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: 98.87%
- CAS 番号: 3034805-75-6
- 分子式: C40H40F2N12O5
- 分子量:806.82
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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生物活性
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PLK4 8.4 nM (IC50) |
PLK4 19.5 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.073 μM
Compound: SP27
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Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 assay
Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 assay
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[PMID: 37279162] |
SP27 potently binds to purified PLK4 protein with an IC50 of 8.4 nM; it potently inhibits the proliferation of TRIM37-amplified MCF-7 breast cancer cells with an IC50 of 0.073 μM[1].
SP27 exhibits favorable in vitro metabolic stability in human plasma as well as liver microsomes from humans, rats and mice, and shows extremely weak inhibitory effects on major CYP450 isoforms, suggesting a low risk of drug-drug interactions[1].
SP27 (0.1-10 μM; 48 h) induces concentration-dependent degradation of PLK4 in TRIM37-amplified MCF-7 breast cancer cells, with a DC50 of 19.5 nM; it induces PLK4 degradation in TRIM37-amplified MCF-7 breast cancer cells via the CRBN-dependent ubiquitin-proteasome pathway[1].
SP27 inhibits the downstream signaling pathway of PLK4 in TRIM37-amplified MCF-7 breast cancer cells in a concentration-dependent manner by reducing FBXW5 inactivation and promoting SAS-6 degradation[1].
SP27 (1 μM; 48 h) exhibits favorable proteome selectivity for PLK4 in TRIM37-amplified MCF-7 breast cancer cells, and its anti-tumor activity is associated with the p53 signaling pathway[1].
SP27 (0.05-2.00 μM) inhibits colony formation, induces apoptosis and G2 phase cell cycle arrest, promotes cellular senescence (48 h), and suppresses the migration of TRIM37-amplified MCF-7 breast cancer cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TRIM37-amplified MCF-7 breast cancer cells
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Concentration:0.1, 1, 10 μM
1 nM, 3 nM, 10 nM, 300 nM, 1 μM, 3 μM, 10 μM (DC50 test) -
Incubation Time:48 h
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Result:Induced PLK4 degradation in a concentration-dependent manner, with 68.3% degradation at 0.1 μM, 73.4% degradation at 1 μM, and 83.5% degradation at 10 μM after 48 h of treatment.
Achieved a half-maximal degradation concentration (DC50) of 19.5 nM, with no observed hook effect at 10 μM.
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Cell Line:MCF-7 breast cancer cells
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Concentration:0.1, 0.3, 1 μM
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Incubation Time:24, 48 h
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Result:Inhibited the migration of MCF-7 cells in a wound healing assay.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3034805-75-6
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性状 Solid
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分子量 806.82
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分子式 C40H40F2N12O5
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Color Light yellow to yellow
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SMILES
FC1=CC=C(C(F)=C1)CNC2=NC3=C(C=NN3C4CCN(CC4)C(C5CCN(CC5)C6=CC7=C(C=C6)C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=O)C(NC9=NNC(C)=C9)=N2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 100 mg/mL (123.94 mM; Need ultrasonic; 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 (protect from light). 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 (protect from light). 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 (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 | 1.2394 mL | 6.1972 mL | 12.3943 mL | 30.9858 mL |
| 5 mM | 0.2479 mL | 1.2394 mL | 2.4789 mL | 6.1972 mL | |
| 10 mM | 0.1239 mL | 0.6197 mL | 1.2394 mL | 3.0986 mL | |
| 15 mM | 0.0826 mL | 0.4131 mL | 0.8263 mL | 2.0657 mL | |
| 20 mM | 0.0620 mL | 0.3099 mL | 0.6197 mL | 1.5493 mL | |
| 25 mM | 0.0496 mL | 0.2479 mL | 0.4958 mL | 1.2394 mL | |
| 30 mM | 0.0413 mL | 0.2066 mL | 0.4131 mL | 1.0329 mL | |
| 40 mM | 0.0310 mL | 0.1549 mL | 0.3099 mL | 0.7746 mL | |
| 50 mM | 0.0248 mL | 0.1239 mL | 0.2479 mL | 0.6197 mL | |
| 60 mM | 0.0207 mL | 0.1033 mL | 0.2066 mL | 0.5164 mL | |
| 80 mM | 0.0155 mL | 0.0775 mL | 0.1549 mL | 0.3873 mL | |
| 100 mM | 0.0124 mL | 0.0620 mL | 0.1239 mL | 0.3099 mL |
SP27 関連分類
HY-149324 関連分類
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