2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs FAK
  4. BSJ-04-146

BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC50 = 26 nM). BSJ-04-146 achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 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).

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BSJ-04-146

BSJ-04-146 Chemical Structure

CAS No. : 2414478-45-6

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BSJ-04-146 Related Antibodies

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Description

BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC50 = 26 nM). BSJ-04-146 achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 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).

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].

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

BSJ-04-146 Related Antibodies

Western Blot Analysis[1]

Cell Line: PATU-8988T cells
Concentration: 100 nM
Incubation Time: 1 h, 2 h, 4 h, 8 h, 24 h
Result: Induced FAK degradation in PATU-8988T cells and simultaneously significantly reduced pAKT signaling.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast AUCINF_obs Vss_obs
Mice 10 mg/kg i.p. 6.1 h 1 h 747 ng/mL 222533 min·ng/mL 406707 min·ng/mL /
Mice 2 mg/kg i.v. 3.5 h 0.5 h 5897 ng/mL 287736 min·ng/mL 304143 min·ng/mL 0.68 L/kg
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].

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

Animal Model: Two million PATU-8988T cells were suspended in PBS and subcutaneously injected into the right groin of nude female mice to establish a PATU-8988T xenograft model[1].
Dosage: 15 mg/kg, 50 mg/kg
Administration: I.p., once every two days (three times) or once
Result: Significant FAK degradation was induced in the spleen, liver, and lung tissues after 24 hours.
FAK protein levels partially recovered, but the degradation effect persisted (especially in the spleen and liver).
Molecular Weight

955.03

Formula

C50H57F3N8O8
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BSJ-04-146 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BSJ-04-1462414478-45-6PROTACsFAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseFocal Adhesion KinasePROTACpancreatic cancertriple-negative breast cancerTNBCInhibitorinhibitorinhibit

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