PLX-3618
Based on 1 Customer Validation
PLX-3618 is a selective BRD4 molecular glue degrader with a DC50 of 12.2 nM. PLX-3618 promotes the polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the E3 ligase substrate receptor DCAF11. PLX-3618 inhibits the proliferation of various cancer cells and induces apoptosis in acute myeloid leukemia (AML) cells. PLX-3618 can be used in studies related to acute myeloid leukemia (AML).
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- Pureté : 99.72%
- CAS No.: 2851986-76-8
- Formule: C32H27N9O2S
- Masse moléculaire:601.68
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
BRD4 |
In Vitro
PLX-3618 (multiple concentrations; 72 h) is potent at inhibiting proliferation and inducing apoptosis in MV-4-11 cells after 72 hours of treatment[1].
PLX-3618 (multiple concentrations; 14 days) exhibits reduced activity against human megakaryocyte progenitors compared to its antiproliferative activity in MV-4-11 cells, suggesting a wider therapeutic window relative to CPI-0610[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (female, 4-week-old, implanted with 1 × 107 MV-4-11 tumor cells subcutaneously)[1]
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Dosage:5 mg/kg (BRD4 degradation; tumor regression); 10 mg/kg (tumor regression)
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Administration:i.p. (daily; 14 days)
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Result:Induced complete degradation of BRD4 in MV-4-11 tumors, with > 50% loss of BRD4 protein sustained for greater than 24 hours.
Induced significant tumor regression, with tumor volume remaining suppressed near baseline.
Induced more robust tumor regression, with 7 out of 8 mice having no measurable tumor by day 14, corresponding to a 119% tumor growth inhibition (TGI).
Was well tolerated, with minimal changes in body weight over the 14-day treatment period.
Chemical Information
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CAS No. 2851986-76-8
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Appearance Solid
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Masse moléculaire 601.68
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Formule C32H27N9O2S
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Color White to off-white
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SMILES
O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(C5=CC=CC(NC(C6=C7N(C=CC=N7)N=C6)=O)=C5)C=C4)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (166.20 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. 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)
In Vivo:
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 (4.16 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.16 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Pureté et documentation
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Fiche technique (297 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.6620 mL | 8.3101 mL | 16.6201 mL | 41.5503 mL |
| 5 mM | 0.3324 mL | 1.6620 mL | 3.3240 mL | 8.3101 mL | |
| 10 mM | 0.1662 mL | 0.8310 mL | 1.6620 mL | 4.1550 mL | |
| 15 mM | 0.1108 mL | 0.5540 mL | 1.1080 mL | 2.7700 mL | |
| 20 mM | 0.0831 mL | 0.4155 mL | 0.8310 mL | 2.0775 mL | |
| 25 mM | 0.0665 mL | 0.3324 mL | 0.6648 mL | 1.6620 mL | |
| 30 mM | 0.0554 mL | 0.2770 mL | 0.5540 mL | 1.3850 mL | |
| 40 mM | 0.0416 mL | 0.2078 mL | 0.4155 mL | 1.0388 mL | |
| 50 mM | 0.0332 mL | 0.1662 mL | 0.3324 mL | 0.8310 mL | |
| 60 mM | 0.0277 mL | 0.1385 mL | 0.2770 mL | 0.6925 mL | |
| 80 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL | 0.5194 mL | |
| 100 mM | 0.0166 mL | 0.0831 mL | 0.1662 mL | 0.4155 mL |
PLX-3618 Related Classifications
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