BAY-069
Based on 3 publication(s) in Google Scholar
BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer.
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- Purity: 99.54%
- CAS No.: 2639638-66-5
- 화학식: C22H14ClF3N2O3
- 분자량:446.81
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) BAY-069
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Biological Activity
IC50: 31 nM (BCAT1), 153 nM (BCAT2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
1 μM
Compound: 36
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Upregulation of BCAA expression in human MDA-MB-231 cells
Upregulation of BCAA expression in human MDA-MB-231 cells
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[PMID: 36261130] |
| MDA-MB-231 | IC50 |
874 nM
Compound: 36a; BAY-069
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Upregulation of BCAA expression in human MDA-MB-231 cells
Upregulation of BCAA expression in human MDA-MB-231 cells
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[PMID: 36261130] |
BAY-069 (compound 36a) (70 nM-50 μM; 72 h) inhibits cell proliferation of U-87 and MDA-MB-231[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-87 and MDA-MB-231
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Concentration:70 nM-50 μM
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Incubation Time:72 h
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Result:Inhibited cell proliferation of U-87 and MDA-MB-231 with IC50s of 358 nM and 874 nM, respectively.
BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats[1]
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Dosage:0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.
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Administration:i.v. or p.o.; single dosage
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Result:Pharmacokinetic Parameters of BAY-069 in male Wistar rats[1].
CLblood (L/h/kg) Vss (L/kg) t1/2 (h), i.v. AUCnorm (kg·h/L), i.v. AUCnorm (kg·h/L), p.o. F (%), p.o. 0.64 0.25 1.6 2.9 2.5 89
Chemical Information
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CAS No. 2639638-66-5
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Appearance Solid
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분자량 446.81
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화학식 C22H14ClF3N2O3
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Color White to off-white
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SMILES
CC(C=CC=C1)=C1OC2=C(Cl)C3=C(C=CC=C3)C(N4C(NC(C(F)(F)F)=CC4=O)=O)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
MFSD1 with its accessory subunit GLMP functions as a general dipeptide uniporter in lysosomes. [Abstract]2024 Jul;26(7):1047-1061. PMID: 38839979 -
Research (Wash D C)
Vascular Smooth Muscle Cell-Specific BCAT2 Deficiency Attenuates Diabetic Atherosclerotic Calcification via Histone Propionylation. [Abstract]2026 Jan 6:9:1052. PMID: 41503231 -
용액&용해도
DMSO : 100 mg/mL (223.81 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 (5.60 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.
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.
순도&문서
References
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 | 2.2381 mL | 11.1904 mL | 22.3809 mL | 55.9522 mL |
| 5 mM | 0.4476 mL | 2.2381 mL | 4.4762 mL | 11.1904 mL | |
| 10 mM | 0.2238 mL | 1.1190 mL | 2.2381 mL | 5.5952 mL | |
| 15 mM | 0.1492 mL | 0.7460 mL | 1.4921 mL | 3.7301 mL | |
| 20 mM | 0.1119 mL | 0.5595 mL | 1.1190 mL | 2.7976 mL | |
| 25 mM | 0.0895 mL | 0.4476 mL | 0.8952 mL | 2.2381 mL | |
| 30 mM | 0.0746 mL | 0.3730 mL | 0.7460 mL | 1.8651 mL | |
| 40 mM | 0.0560 mL | 0.2798 mL | 0.5595 mL | 1.3988 mL | |
| 50 mM | 0.0448 mL | 0.2238 mL | 0.4476 mL | 1.1190 mL | |
| 60 mM | 0.0373 mL | 0.1865 mL | 0.3730 mL | 0.9325 mL | |
| 80 mM | 0.0280 mL | 0.1399 mL | 0.2798 mL | 0.6994 mL | |
| 100 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5595 mL |