BIBF0775
Based on 1 Customer Validation
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
For research use only. We do not sell to patients.
- Purity: 99.42%
- CAS No.: 334951-90-5
- Formula: C31H34N4O2
- Molecular Weight:494.63
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
IC50: 34 nM (Alk5)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HaCaT | EC50 |
105 nM
Compound: 5
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Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
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[PMID: 20919678] |
| HaCaT | IC50 |
>1 μM
Compound: 5
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Cytotoxicity against human HaCaT cells
Cytotoxicity against human HaCaT cells
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[PMID: 20919678] |
| HUVEC | EC50 |
718 nM
Compound: 43
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Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay
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[PMID: 19522465] |
| Sf9 | IC50 |
1447 nM
Compound: 43
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Inhibition of human VEGFR2 expressed in Sf9 cells
Inhibition of human VEGFR2 expressed in Sf9 cells
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[PMID: 19522465] |
Chemical Information
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CAS No. 334951-90-5
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Appearance Solid
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Molecular Weight 494.63
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Formula C31H34N4O2
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(C3=CC=CC=C3)\NC4=CC=C(CN5CCCCC5)C=C4)N(CC)C
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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
Solvent & Solubility
DMSO : 62.5 mg/mL (126.36 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 (4.21 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 (4.21 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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.0217 mL | 10.1086 mL | 20.2171 mL | 50.5428 mL |
| 5 mM | 0.4043 mL | 2.0217 mL | 4.0434 mL | 10.1086 mL | |
| 10 mM | 0.2022 mL | 1.0109 mL | 2.0217 mL | 5.0543 mL | |
| 15 mM | 0.1348 mL | 0.6739 mL | 1.3478 mL | 3.3695 mL | |
| 20 mM | 0.1011 mL | 0.5054 mL | 1.0109 mL | 2.5271 mL | |
| 25 mM | 0.0809 mL | 0.4043 mL | 0.8087 mL | 2.0217 mL | |
| 30 mM | 0.0674 mL | 0.3370 mL | 0.6739 mL | 1.6848 mL | |
| 40 mM | 0.0505 mL | 0.2527 mL | 0.5054 mL | 1.2636 mL | |
| 50 mM | 0.0404 mL | 0.2022 mL | 0.4043 mL | 1.0109 mL | |
| 60 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8424 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2527 mL | 0.6318 mL | |
| 100 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5054 mL |