BI-3663 |
Catalog No.GC65457
One-Click Copy Product Info
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BI-3663은 고도로 선택적인 PTK2/FAK PROTAC(DC50=30 nM)이며 Cereblon 리간드가 PTK2 분해를 위해 E3 리가아제를 가로채고 있습니다. BI-3663은 18nM의 IC50으로 PTK2를 억제합니다. BI-3663은 포말리도마이드에 링커로 연결된 BI-4464로 구성된 PROTAC이다. 항암 활성.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2341740-84-7
Sample solution is provided at 25 µL, 10mM.
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BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 linked to Pomalidomide with a linker[1]. Anti-cancer activity[1].
BI-3663 potently degrades PTK2 in Hep3B2.1-7 cells, and A549 cells, with pDC50s of 7.6 and 7.9, respectively[1].
[1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.
PTK2/FAK 18nM(IC50) | Cereblon
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| Cas No. | 2341740-84-7 | SDF | |
| Formula | C44H42F3N7O12 | M.Wt | 917.84 |
| Solubility | DMSO : 300 mg/mL (326.85 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0895 mL | 5.4476 mL | 10.8951 mL |
| 5 mM | 217.9 μL | 1.0895 mL | 2.179 mL |
| 10 mM | 109 μL | 544.8 μL | 1.0895 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)