BI-3663
Based on 1 publication(s) in Google Scholar
BI-3663 is a highly selective PTK2/FAK PROTAC (DC50 = 30 nM) with a Cereblon E3 ligase ligand capable of degrading PTK2, with an IC50 value of 18 nM. BI-3663 is a PROTAC generated by linking the PTK2/FAK inhibitor BI-4464 (HY-124625) with a Pomalidomide (HY-10984) derivative via a linker. BI-3663 can induce PTK2 degradation at low nanomolar concentrations. BI-3663 has antitumor activity.
(Pink: FAK ligand (HY-43760); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42490)).
Para uso exclusivo en investigación. No vendemos a pacientes.
The BI-3663 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.
- Pureza: 99.84%
- No. CAS: 2341740-84-7
- Fòrmula: C44H42F3N7O12
- Peso molecular:917.84
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Heterocyclic Compound Library
HY-L138
-
PROTAC Library
HY-L151
-
Highly Selective Inhibitors Library
HY-L158
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) BI-3663
MoreVer todos los productos específicos de isoformas PROTACs
More
Actividad biológica
|
PTK2/FAK 18 nM (IC50) |
Cereblon |
BI-3663 potently degrades PTK2 in Hep3B2.1-7 cells, and A549 cells, with pDC50s of 7.6 and 7.9, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 2341740-84-7
-
Appearance Solid
-
Peso molecular 917.84
-
Fòrmula C44H42F3N7O12
-
Color Light yellow to yellow
-
SMILES
O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCOCCOCCOCCNC(C4=CC=C(NC5=NC=C(C(F)(F)F)C(OC6=CC=CC(CC7)=C6C7=O)=N5)C(OC)=C4)=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Solvente y solubilidad
DMSO : 300 mg/mL (326.85 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: ≥ 7.5 mg/mL (8.17 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Ficha de datos (270 KB)
-
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)
-
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, 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 | 1.0895 mL | 5.4476 mL | 10.8951 mL | 27.2379 mL |
| 5 mM | 0.2179 mL | 1.0895 mL | 2.1790 mL | 5.4476 mL | |
| 10 mM | 0.1090 mL | 0.5448 mL | 1.0895 mL | 2.7238 mL | |
| 15 mM | 0.0726 mL | 0.3632 mL | 0.7263 mL | 1.8159 mL | |
| 20 mM | 0.0545 mL | 0.2724 mL | 0.5448 mL | 1.3619 mL | |
| 25 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 30 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9079 mL | |
| 40 mM | 0.0272 mL | 0.1362 mL | 0.2724 mL | 0.6809 mL | |
| 50 mM | 0.0218 mL | 0.1090 mL | 0.2179 mL | 0.5448 mL | |
| 60 mM | 0.0182 mL | 0.0908 mL | 0.1816 mL | 0.4540 mL | |
| 80 mM | 0.0136 mL | 0.0681 mL | 0.1362 mL | 0.3405 mL | |
| 100 mM | 0.0109 mL | 0.0545 mL | 0.1090 mL | 0.2724 mL |
BI-3663 Related Classifications
HY-111546 Related Classifications
Powered by Bioz