BMS-605541
Based on 1 Customer Validation
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.57%
- CAS. Nr.: 639858-32-5
- Formel: C19H17F2N5OS
- Molecular Weight:401.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Alle VEGFR Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
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VEGFR-2 23 nM (IC50) |
VEGFR-2 49 nM (Ki) |
Flk-1 40 nM (IC50) |
VEGFR-1 400 nM (IC50) |
PDGFR-β 200 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
16.6 μM
Compound: 14
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Inhibition of human ERG expressed in HEK293 cells
Inhibition of human ERG expressed in HEK293 cells
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[PMID: 16789733] |
| HUVEC | IC50 |
25 nM
Compound: 14
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Antiproliferative activity against VEGF-stimulated HUVEC
Antiproliferative activity against VEGF-stimulated HUVEC
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[PMID: 16789733] |
| L2987 | IC50 |
>2500 nM
Compound: 14
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Antiproliferative activity against L2987 cells
Antiproliferative activity against L2987 cells
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[PMID: 16789733] |
Pharmacokinetic (PK) parameters of BMS-605541[1]
| Species | Administration manner | Dose (mg/kg) | Cmax (μM) | Tmax (h) | AUC (μM h) | T1/2 (h) | MRT (h) | Cl (mL/min kg) | Vss (L/kg) | Fpo (%) |
| Mouse | Oral gavage | 90 | 148 | 0.5 | 649 (0-24 h) | 1.7 | 3.4 | 100 | ||
| Mouse | Intravenous injection | 10 | 11.8 | 1.7 | 100 | |||||
| Rat | Oral gavage | 50 | 44.0 | 2.0 | 202 | 2.2 | 3.5 | 100 | ||
| Rat | Intravenous injection | 10 | 13.6 | 1.1 | 100 | |||||
| Cyno | Oral gavage | 5 | 8.0 | 0.75 | 28.5 | 7.1 | 7.9 | 52 | ||
| Cyno | Intravenous injection | 1 | 3.9 | 1.6 | 52 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 639858-32-5
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Appearance Solid
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Molecular Weight 401.43
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Formel C19H17F2N5OS
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Color White to off-white
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SMILES
FC1=C(C=C(C(F)=C1)C(NC2CC2)=O)NCC3=CN=C(S3)NC4=NC=CC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 33.33 mg/mL (83.03 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.18 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.
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.
Reinheit & Dokumentation
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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)
Verweise
[1]. Borzilleri RM, et al. Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. J Med Chem. 2006 Jun 29;49(13):3766-9. [Content Brief]
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 | 2.4911 mL | 12.4555 mL | 24.9109 mL | 62.2774 mL |
| 5 mM | 0.4982 mL | 2.4911 mL | 4.9822 mL | 12.4555 mL | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4911 mL | 6.2277 mL | |
| 15 mM | 0.1661 mL | 0.8304 mL | 1.6607 mL | 4.1518 mL | |
| 20 mM | 0.1246 mL | 0.6228 mL | 1.2455 mL | 3.1139 mL | |
| 25 mM | 0.0996 mL | 0.4982 mL | 0.9964 mL | 2.4911 mL | |
| 30 mM | 0.0830 mL | 0.4152 mL | 0.8304 mL | 2.0759 mL | |
| 40 mM | 0.0623 mL | 0.3114 mL | 0.6228 mL | 1.5569 mL | |
| 50 mM | 0.0498 mL | 0.2491 mL | 0.4982 mL | 1.2455 mL | |
| 60 mM | 0.0415 mL | 0.2076 mL | 0.4152 mL | 1.0380 mL | |
| 80 mM | 0.0311 mL | 0.1557 mL | 0.3114 mL | 0.7785 mL |
BMS-605541 Related Classifications
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