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Cat. No.: HY-179512A

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BSJ-04-146 tetraTFA

Name: BSJ-04-146 tetraTFA
Brand: MedChemExpress
SKU: HY-179512A
Price: 590.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Based on 1 Customer Validation

BSJ-04-146 tetraTFA is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC₅₀ = 26 nM). BSJ-04-146 tetraTFA achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 tetraTFA binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 tetraTFA can be used for the study of pancreatic cancer and triple-negative breast cancer.
(Pink: FAK ligand (HY-151010); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W011561)).

For research use only. We do not sell to patients.

Formula: C₅₈H₆₁F₁₅N₈O₁₆
Molecular Weight:1411.12

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

BSJ-04-146 tetraTFA Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
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Biological Activity

Description

BSJ-04-146 tetraTFA is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC₅₀ = 26 nM). BSJ-04-146 tetraTFA achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 tetraTFA binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 tetraTFA can be used for the study of pancreatic cancer and triple-negative breast cancer^[1]. (Pink: FAK ligand (HY-151010); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W011561)).

All PROTACs Isoforms :

In Vitro

BSJ-04-146 (1-1000 nM, 4 h) tetraTFA can efficiently degrade FAK protein in PATU-8988T cells^[1].
BSJ-04-146 (100 nM, 1-24 h) tetraTFA can rapidly induce FAK degradation in PATU-8988T cells and simultaneously significantly reduce pAKT signaling^[1].
BSJ-04-146 (120 h) tetraTFA significantly inhibits the 3D spheroid viability of PATU-8988T and MDA-MB-231 cells^[1].
BSJ-04-146 (100 nM, 4-24 h) tetraTFA 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BSJ-04-146 (15-50 mg/kg, i.p., once every two days (three times) or once) tetraTFA can induce durable and systemic FAK degradation in PATU-8988T cell xenograft mice and is well tolerated in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Breast Cancer Modeling

Chemical Information

Appearance Solid
Molecular Weight 1411.12
Formula C₅₈H₆₁F₁₅N₈O₁₆
SMILES

O=C(NC)C1=CC=CC=C1NC2=CC(NC3=CC(C)=C(C4CCN(CCCCCCNC(COC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3OC(C)C)=NC=C2C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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