JET-209
Based on 1 Customer Validation
JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia.
(Pink: CBP/p300 Target protein ligand; Blue: Cereblon ligand (HY-132248); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.27%
- No. CAS: 3033714-58-5
- Fòrmula: C46H47N9O6
- Peso molecular:821.92
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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CBP 0.05 nM (DC50) |
p300 0.2 nM (DC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
0.54 nM
Compound: 24; JET-209
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Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
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[PMID: 37276143] |
| MOLM-13 | IC50 |
2.3 nM
Compound: 24; JET-209
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Cytotoxicity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
Cytotoxicity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
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[PMID: 37276143] |
| MV4-11 | IC50 |
0.04 nM
Compound: 24; JET-209
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Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
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[PMID: 37276143] |
| RS4-11 | IC50 |
0.1 nM
Compound: 24; JET-209
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Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
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[PMID: 37276143] |
JET-209 exhibits strong antiproliferative activity against MV4;11 (IC50 = 0.04 nM), HL-60 (IC50 = 0.54 nM), MOLM-13 (IC50 = 2.3 nM) and RS4;11 cells (IC50 = 0.1 nM)[1].
JET-209 (1 nM- 1 μM, 24 h) effectively induces G1 phase arrest in RS4;11 cells[1].
FIP22 (1 nM- 1 μM, 8 h) potently and effectively suppresses the expression ofMYC and MYB genes in the RS4;11 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11 cells
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:24 h
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Result:Effectively induced G1 arrest at concentrations as low as 1 nM.
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Cell Line:RS4;11 cells
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:8 h
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Result:Effectively suppressed the expression ofMYC and MYB genes.
JET-209 (0.3-3 mg/kg, i.p., for 2 weeks) achieves strong tumor inhibition in RS4;11 and MV4;11 xenograft tumor mice models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:RS4;11 cells xenograft model established in female immunodeficient (SCID) mice[1]
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Dosage:1 and 3 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose, twice a week (1 mg/kg) or once a week (3 mg/kg) for 2 weeks
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Result:Completely eliminated the CBP/p300 protein in the tumor within 3 to 6 hours at a single administration, and the protein level returned to normal 24 hours later.
Achieved 81% long-term tumor growth inhibition with continuous administration at 3 mg/kg.
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Animal Model:MV4;11 cells xenograft model established in female immunodeficient (SCID) mice[1]
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Dosage:0.3 and 1 mg/kg
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Administration:Intraperitoneal injection (i.p.), 0.3 mg/kg once daily 5 days a week for 2 weeks or 1 mg/kg three times a week for 2 weeks
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Result:Demonstrated potent anti-tumor activity and has good safety profile.
Chemical Information
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No. CAS 3033714-58-5
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Appearance Solid
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Peso molecular 821.92
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Fòrmula C46H47N9O6
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Color Light yellow to yellow
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SMILES
CC(N1CCC2=C(C(C3=CC=CC4=C3C=NC(C5=CN=C(C=C5)C(NC6CCN(CC6)C7=CC8=C(C(N(C8)C9CCC(NC9=O)=O)=O)C=C7)=O)=C4)=NN2C%10CCOCC%10)C1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (121.67 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)
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 (3.04 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (3.04 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.2167 mL | 6.0833 mL | 12.1666 mL | 30.4166 mL |
| 5 mM | 0.2433 mL | 1.2167 mL | 2.4333 mL | 6.0833 mL | |
| 10 mM | 0.1217 mL | 0.6083 mL | 1.2167 mL | 3.0417 mL | |
| 15 mM | 0.0811 mL | 0.4056 mL | 0.8111 mL | 2.0278 mL | |
| 20 mM | 0.0608 mL | 0.3042 mL | 0.6083 mL | 1.5208 mL | |
| 25 mM | 0.0487 mL | 0.2433 mL | 0.4867 mL | 1.2167 mL | |
| 30 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0139 mL | |
| 40 mM | 0.0304 mL | 0.1521 mL | 0.3042 mL | 0.7604 mL | |
| 50 mM | 0.0243 mL | 0.1217 mL | 0.2433 mL | 0.6083 mL | |
| 60 mM | 0.0203 mL | 0.1014 mL | 0.2028 mL | 0.5069 mL | |
| 80 mM | 0.0152 mL | 0.0760 mL | 0.1521 mL | 0.3802 mL | |
| 100 mM | 0.0122 mL | 0.0608 mL | 0.1217 mL | 0.3042 mL |
JET-209 Related Classifications
HY-154984 Related Classifications
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