BI-4924
Based on 1 publication(s) in Google Scholar
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
For research use only. We do not sell to patients.
The BI-4924 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Purity: 99.55%
- CAS No.: 2244452-09-1
- Formula: C21H20Cl2N2O6S
- Molecular Weight:499.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BI-4924
More
Biological Activity
PHGDH[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-468 | IC50 |
2200 nM
Compound: BI-4924
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Inhibition of PHGDH in human MDA-MB-468 cells assessed as reduction in [13C]-serine incubated for 72 hrs using [13C]glucose as substrate by LC-MS/MS analysis
Inhibition of PHGDH in human MDA-MB-468 cells assessed as reduction in [13C]-serine incubated for 72 hrs using [13C]glucose as substrate by LC-MS/MS analysis
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[PMID: 31365252] |
BI-4924 is a highly potent co-factor nicotinamide adenine dinucleotide (NADH/NAD+)-competitive PHGDH inhibitor. BI-4924 shows high selectivity against the majority of other dehydrogenase targets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2244452-09-1
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Appearance Solid
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Molecular Weight 499.36
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Formula C21H20Cl2N2O6S
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Color Off-white to yellow
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SMILES
O=C(O)CS(=O)(C1=CC=C([C@H](NC(C(N2C)=CC3=C2C=C(C)C(Cl)=C3Cl)=O)CO)C=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Purine nucleotide depletion prompts cell migration by stimulating the serine synthesis pathway. [Abstract]2022 May 16;13(1):2698. PMID: 35577785
Solvent & Solubility
DMSO : 125 mg/mL (250.32 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
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Data Sheet (274 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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Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0026 mL | 10.0128 mL | 20.0256 mL | 50.0641 mL |
| 5 mM | 0.4005 mL | 2.0026 mL | 4.0051 mL | 10.0128 mL | |
| 10 mM | 0.2003 mL | 1.0013 mL | 2.0026 mL | 5.0064 mL | |
| 15 mM | 0.1335 mL | 0.6675 mL | 1.3350 mL | 3.3376 mL | |
| 20 mM | 0.1001 mL | 0.5006 mL | 1.0013 mL | 2.5032 mL | |
| 25 mM | 0.0801 mL | 0.4005 mL | 0.8010 mL | 2.0026 mL | |
| 30 mM | 0.0668 mL | 0.3338 mL | 0.6675 mL | 1.6688 mL | |
| 40 mM | 0.0501 mL | 0.2503 mL | 0.5006 mL | 1.2516 mL | |
| 50 mM | 0.0401 mL | 0.2003 mL | 0.4005 mL | 1.0013 mL | |
| 60 mM | 0.0334 mL | 0.1669 mL | 0.3338 mL | 0.8344 mL | |
| 80 mM | 0.0250 mL | 0.1252 mL | 0.2503 mL | 0.6258 mL | |
| 100 mM | 0.0200 mL | 0.1001 mL | 0.2003 mL | 0.5006 mL |
BI-4924 Related Classifications
HY-126254 Related Classifications
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