BSJ-04-146 |
Catalog No.GC81301
One-Click Copy Product Info
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BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase ( FAK ) inhibitor( IC50 = 26 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2414478-45-6
Sample solution is provided at 25 µL, 10mM.
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In Vivo, BSJ-04-146 (15-50 mg/kg, i.p., once every two days (three times) or once) can induce durable and systemic FAK degradation in PATU-8988T cell xenograft mice and is well tolerated in mice[1].
In Vitro, BSJ-04-146 (1-1000 nM, 4 h) can efficiently degrade FAK protein in PATU-8988T cells[1]. BSJ-04-146 (100 nM, 1-24 h) can rapidly induce FAK degradation in PATU-8988T cells and simultaneously significantly reduce pAKT signaling[1]. BSJ-04-146 (120 h) significantly inhibits the 3D spheroid viability of PATU-8988T and MDA-MB-231 cells[1]. BSJ-04-146 (100 nM, 4-24 h) induced significant changes in 74 pY and 161 pY-IMAC phosphopeptides in PATU-8988T cells (including downregulation of FAK autophosphorylation sites); the changes persisted after 24 hours of treatment[1].
References:
[1]. Koide E, et al. Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity. Chembiochem. 2023 Oct 4;24(19):e202300141.
| Cas No. | 2414478-45-6 | SDF | |
| Formula | C50H57F3N8O8 | M.Wt | 955.03 |
| Solubility | Storage | Store at -20°C | |
| 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 | 1.0471 mL | 5.2354 mL | 10.4709 mL |
| 5 mM | 209.4 μL | 1.0471 mL | 2.0942 mL |
| 10 mM | 104.7 μL | 523.5 μL | 1.0471 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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: >98.00% 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.)