BTX-A51
Based on 2 publication(s) in Google Scholar
BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.99%
- No. CAS: 2079068-74-7
- Fòrmula: C18H25ClN6
- Peso molecular:360.88
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BTX-A51
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CK1α/CSNK1A1 |
CDK7 1.3 nM (Kd) |
CDK9 4 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
158.5 nM
Compound: BTX-A51
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 39140066] |
| T-cell | IC50 |
4 nM
Compound: 12; BTX-A51
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Inhibition of CDK9/Cyclin T (unknown origin)
Inhibition of CDK9/Cyclin T (unknown origin)
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[PMID: 35485642] |
In Vitro
Similar to CKIα depletion, BTX-A51 (0.05-3.2 μM; 18 hours) treatment of RKO cells abolished most of the Ser45 phosphorylation signal and the consecutive GSK3 phosphorylation cascade resulting in stabilization of β-catenin[1].
BTX-A51 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53[1].
BTX-A51 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. BTX-A51 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.08 μM, 0.6 μM, 2 μM
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Incubation Time:6.5 hours
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Result:Abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1.
In Vivo
Pharmacokinetic studies of the inhibitor BTX-A51 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.5-2 hr, Cmax of 1060 ng/mL, T1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2079068-74-7
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Appearance Solid
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Peso molecular 360.88
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Fòrmula C18H25ClN6
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Color White to light yellow
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SMILES
N[C@H]1CC[C@H](NC2=NC=C(Cl)C(C3=C(CC4CC4)N(C)N=C3)=N2)CC1
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Synonyms
Casein Kinase inhibitor A51
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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 (2)
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Journal Impact Factor
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Most Recent
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Leukemia
Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]2025 Sep;39(9):2163-2173. PMID: 40670672 -
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (277.10 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 (6.93 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 (6.93 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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 2.7710 mL | 13.8550 mL | 27.7100 mL | 69.2751 mL |
| 5 mM | 0.5542 mL | 2.7710 mL | 5.5420 mL | 13.8550 mL | |
| 10 mM | 0.2771 mL | 1.3855 mL | 2.7710 mL | 6.9275 mL | |
| 15 mM | 0.1847 mL | 0.9237 mL | 1.8473 mL | 4.6183 mL | |
| 20 mM | 0.1386 mL | 0.6928 mL | 1.3855 mL | 3.4638 mL | |
| 25 mM | 0.1108 mL | 0.5542 mL | 1.1084 mL | 2.7710 mL | |
| 30 mM | 0.0924 mL | 0.4618 mL | 0.9237 mL | 2.3092 mL | |
| 40 mM | 0.0693 mL | 0.3464 mL | 0.6928 mL | 1.7319 mL | |
| 50 mM | 0.0554 mL | 0.2771 mL | 0.5542 mL | 1.3855 mL | |
| 60 mM | 0.0462 mL | 0.2309 mL | 0.4618 mL | 1.1546 mL | |
| 80 mM | 0.0346 mL | 0.1732 mL | 0.3464 mL | 0.8659 mL | |
| 100 mM | 0.0277 mL | 0.1386 mL | 0.2771 mL | 0.6928 mL |
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