BTX161
Based on 1 publication(s) in Google Scholar
BTX161, a Thalidomide (HY-14658) analog, is a molecular glue degrader targeting CK1α. BTX161 recruits CK1α and the CK1α-FAM83 complex to the Cul4ACRBN E3 ligase complex, thereby driving ubiquitination and proteasomal degradation. BTX161 reduces FAM83G abundance through CK1α-FAM83G co-stability, slightly decreases FAM83H levels, but has no effect on the expression of FAM83B. BTX161 activates DNA damage response (DDR) and upregulates Wnt target genes including MYC. BTX161 can be used in research related to colorectal cancer, type b myelomonocytic leukemia and acute myeloid leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.20%
- No. CAS: 2052301-24-1
- Fòrmula: C15H16N2O3
- Peso molecular:272.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BTX161
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CK1α |
In Vitro
BTX161 (0.1-10 μM; 6-24 h) induces robust, time- and dose-dependent degradation of CK1α in HCT116, DLD-1, and MV4.11 cells, and induces degradation of FAM83F in HCT116 and DLD-1 cells, with optimal activity observed at 10 μM for 24 h; it also reduces FAM83H and FAM83G levels in select cell lines[1].
BTX161 (10 μM; 24 h) potently depletes SACK1F but does not degrade CK1α, SACK1B, SACK1G, or SACK1H in wild-type DLD1 human colorectal cancer cells[2].
BTX161 induces CKIα degradation, activates DDR and p53, stabilizes MDM2, and upregulates Wnt target gene expression in human AML MV4-11 cells[3].
BTX161 synergizes with CDK7 and CDK9 inhibitors to enhance p53 activation and caspase 3-mediated apoptosis in human AML MV4-11 cells[3].
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:HCT116 colorectal cancer cells, DLD-1 colorectal cancer cells, MV4.11 B-myelomonocytic leukaemia cells
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:6, 16, 24 h
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Result:Induced robust degradation of FAM83F and CK1α in HCT116 and DLD-1 cells in a time- and dose-dependent manner, with optimal degradation observed at 10 μM for 24 h.
Caused substantial degradation of CK1α in MV4.11 cells, with near-complete depletion observed at 10 μM for 24 h.
Slightly reduced FAM83H protein abundance in HCT116 and MV4.11 cells treated with 10 μM for 24 h.
Slightly reduced FAM83G protein abundance in DLD-1 cells and almost fully depleted FAM83G in MV4.11 cells treated with 10 μM for 24 h.
Left FAM83B protein levels unaffected across all cell lines.
Chemical Information
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No. CAS 2052301-24-1
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Appearance Solid
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Peso molecular 272.30
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Fòrmula C15H16N2O3
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Color White to off-white
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SMILES
O=C([C@@H](N(CC1=C2C=CC=C1C)C2=O)CCC3)NC3=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (91.81 mM; ultrasonic and warming and heat to 60°C; 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 (9.18 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 (9.18 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.
Protocolo
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Pureza y Documentación
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Ficha de datos (289 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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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 | 3.6724 mL | 18.3621 mL | 36.7242 mL | 91.8105 mL |
| 5 mM | 0.7345 mL | 3.6724 mL | 7.3448 mL | 18.3621 mL | |
| 10 mM | 0.3672 mL | 1.8362 mL | 3.6724 mL | 9.1811 mL | |
| 15 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL | 6.1207 mL | |
| 20 mM | 0.1836 mL | 0.9181 mL | 1.8362 mL | 4.5905 mL | |
| 25 mM | 0.1469 mL | 0.7345 mL | 1.4690 mL | 3.6724 mL | |
| 30 mM | 0.1224 mL | 0.6121 mL | 1.2241 mL | 3.0604 mL | |
| 40 mM | 0.0918 mL | 0.4591 mL | 0.9181 mL | 2.2953 mL | |
| 50 mM | 0.0734 mL | 0.3672 mL | 0.7345 mL | 1.8362 mL | |
| 60 mM | 0.0612 mL | 0.3060 mL | 0.6121 mL | 1.5302 mL | |
| 80 mM | 0.0459 mL | 0.2295 mL | 0.4591 mL | 1.1476 mL |
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