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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- CAS No.: 2414478-45-6
- Formule: C50H57F3N8O8
- Masse moléculaire:955.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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.
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Cell Line:PATU-8988T cells
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Concentration:100 nM
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Incubation Time:1 h, 2 h, 4 h, 8 h, 24 h
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Result:Induced FAK degradation in PATU-8988T cells and simultaneously significantly reduced pAKT signaling.
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:15 mg/kg, 50 mg/kg
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Administration:I.p., once every two days (three times) or once
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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).
Chemical Information
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CAS No. 2414478-45-6
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Masse moléculaire 955.03
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Formule C50H57F3N8O8
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BSJ-04-146 Related Classifications
HY-179512 Related Classifications
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