PET-16
Based on 1 Customer Validation
PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma.
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- 純度 : 98.07%
- CAS 番号: 34387-64-9
- 分子式: C26H20BrP
- 分子量:443.31
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
PET-16 (0.01-100 μM; 72 h) shows cytotoxicity in Multiple myeloma (MM) cell lines with the highest steady-state level of HSP70 showed the lowest IC50[1].
PET-16 (3 μM; 24 h) induces apoptosis in multiple myeloma, along with proteotoxic stress[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:U266, H929, MM1.S, RPMI-8226 and OCI-MY5 cells
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Concentration:0.01 μM, 0.1 μM, 1 μM.10 μM, 100 μM
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Incubation Time:72 h
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Result:All of the MM lines showed cytotoxicity.
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Cell Line:U266, H929, MM1.S, RPMI-8226 and OCI-MY5 cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Induced apoptosis in treated cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice injected with 1205Lu human melanoma cells[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:i.p. injection; twice a week; for 3 weeks
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Result:Markedly decreased p-FAK and BRAF staining.
化学情報
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CAS 番号 34387-64-9
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性状 Solid-Liquid Mixture
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分子量 443.31
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分子式 C26H20BrP
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Color Light yellow to yellow
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SMILES
C1(C#C[P+](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)=CC=CC=C1.[Br-]
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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, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (225.58 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
純度とドキュメンテーション
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データシート (276 KB)
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SDS (394 KB)
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- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Charvann K Bailey, et al. Efficacy of the HSP70 inhibitor PET-16 in multiple myeloma. Cancer Biol Ther. 2015;16(9):1422-6. [Content Brief]
[2]. Anna Budina-Kolomets, et al. HSP70 Inhibition Limits FAK-Dependent Invasion and Enhances the Response to Melanoma Treatment with BRAF Inhibitors. Cancer Res. 2016 May 1;76(9):2720-30. [Content Brief]
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 (sealed storage, away from moisture and 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 | 2.2558 mL | 11.2788 mL | 22.5576 mL | 56.3939 mL |
| 5 mM | 0.4512 mL | 2.2558 mL | 4.5115 mL | 11.2788 mL | |
| 10 mM | 0.2256 mL | 1.1279 mL | 2.2558 mL | 5.6394 mL | |
| 15 mM | 0.1504 mL | 0.7519 mL | 1.5038 mL | 3.7596 mL | |
| 20 mM | 0.1128 mL | 0.5639 mL | 1.1279 mL | 2.8197 mL | |
| 25 mM | 0.0902 mL | 0.4512 mL | 0.9023 mL | 2.2558 mL | |
| 30 mM | 0.0752 mL | 0.3760 mL | 0.7519 mL | 1.8798 mL | |
| 40 mM | 0.0564 mL | 0.2820 mL | 0.5639 mL | 1.4098 mL | |
| 50 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1279 mL | |
| 60 mM | 0.0376 mL | 0.1880 mL | 0.3760 mL | 0.9399 mL | |
| 80 mM | 0.0282 mL | 0.1410 mL | 0.2820 mL | 0.7049 mL | |
| 100 mM | 0.0226 mL | 0.1128 mL | 0.2256 mL | 0.5639 mL |
PET-16 関連分類
HY-122184 関連分類
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