PLX-4104
Based on 1 Customer Validation
PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia.
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- Pureté : 98.24%
- CAS No.: 2851986-77-9
- Formule: C32H26FN9O2S
- Masse moléculaire:619.67
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
BRD4 2 nM (DC50) |
DCAF11 |
In Vitro
PLX-4104 potently binds to BRD4 with an IC50 of 4 nM[1].
PLX-4104 (24 h) induces near-complete (>95%) BRD4 degradation in MV-4-11 cells with a DC50 of 2 nM[1].
PLX-4104 (72 h) potently inhibits the proliferation of MV-4-11 cells with an EC50 of 4 nM[1].
PLX-4104 has intrinsic clearance of 11.1 mL/min/kg in human liver microsomes and <10 mL/min/kg in mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | T1/2 | Vss | AUC0-inf | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 16.6 mL/min/kg | 1.2 h | 1.1 L/kg | / | / | / | / |
| Mice[1] | 50 mg/kg | p.o. | / | / | / | 19.0 μM·h | 6.74 μM | 2.0 h | 23 % |
| Rat[1] | 1 mg/kg | i.v. | 8.1 mL/min/kg | 1.1 h | 0.6 L/kg | / | / | / | / |
| Rat[1] | 10 mg/kg | p.o. | / | / | / | 3.7 μM·h | 0.87 μM | 2.0 h | 11 % |
| Dog[1] | 1 mg/kg | i.v. | 2.5 mL/min/kg | 2.8 h | 0.5 L/kg | / | / | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | / | 8.0 μM·h | 1.49 μM | 1.7 h | 14 % |
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 mice with AML MV-4-11 xenografts[1]
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Dosage:2 mg/kg; 6 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Achieved approximately 50% tumor growth inhibition (TGI) by day 21 (2 mg/kg).
Achieved complete tumor regression, with no measurable tumors detected on day 21 (6 mg/kg).
Caused no significant changes in mouse body weight with either dose.
Chemical Information
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CAS No. 2851986-77-9
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Appearance Solid
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Masse moléculaire 619.67
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Formule C32H26FN9O2S
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Color White to off-white
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SMILES
O=C(NC1=C(F)C=CC(C2=CC=C(C3=N[C@@H](CC(N)=O)C4=NN=C(C)N4C5=C3C(C)=C(C)S5)C=C2)=C1)C6=C7N=CC=CN7N=C6
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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 (161.38 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 (4.03 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 (4.03 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 (280 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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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6138 mL | 8.0688 mL | 16.1376 mL | 40.3441 mL |
| 5 mM | 0.3228 mL | 1.6138 mL | 3.2275 mL | 8.0688 mL | |
| 10 mM | 0.1614 mL | 0.8069 mL | 1.6138 mL | 4.0344 mL | |
| 15 mM | 0.1076 mL | 0.5379 mL | 1.0758 mL | 2.6896 mL | |
| 20 mM | 0.0807 mL | 0.4034 mL | 0.8069 mL | 2.0172 mL | |
| 25 mM | 0.0646 mL | 0.3228 mL | 0.6455 mL | 1.6138 mL | |
| 30 mM | 0.0538 mL | 0.2690 mL | 0.5379 mL | 1.3448 mL | |
| 40 mM | 0.0403 mL | 0.2017 mL | 0.4034 mL | 1.0086 mL | |
| 50 mM | 0.0323 mL | 0.1614 mL | 0.3228 mL | 0.8069 mL | |
| 60 mM | 0.0269 mL | 0.1345 mL | 0.2690 mL | 0.6724 mL | |
| 80 mM | 0.0202 mL | 0.1009 mL | 0.2017 mL | 0.5043 mL | |
| 100 mM | 0.0161 mL | 0.0807 mL | 0.1614 mL | 0.4034 mL |
PLX-4104 Related Classifications
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