BJ-2302
BJ-2302 is a Src kinase inhibitor with an IC50 of 3.23 μM, and inhibits cathepsin S (CTSS) activity.BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression.BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth.BJ-2302 does not induce cytotoxicity in normal breast epithelial cells.BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer.
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- CAS. Nr.: 1631056-29-5
- Formel: C9H10N2O2
- Molecular Weight:178.19
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
BJ-2302 inhibits Src-regulated PI3K/AKT and Ras/Raf/ERK signaling pathways in MDA-MB-231 cells, and suppresses the invasion of MDA-MB-231 cells[1].
BJ-2302 (0.01-10 µM; 18 h) inhibits serum-induced invasion of MDA-MB-231 triple-negative breast cancer (TNBC) cells, with an IC50 of 0.08 µM and an IC90 of 0.71 µM[3].
BJ-2302 (0.01-10 µM) downregulates the mRNA and protein expression of basal CTSS and MMP-9 in MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner[3].
BJ-2302 (0.01-1 µM) inhibits the nuclear translocation of NF-κB, and suppresses the phosphorylation of PI3K/Akt as well as the phosphorylation of molecules in the Ras/Raf/ERK pathway in a concentration-dependent manner in vitro in MDA-MB-231 triple-negative breast cancer (TNBC) cells[3].
BJ-2302 (0.01-10 µM; 73 h) inhibits serum-induced proliferation of MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, and achieves complete inhibition of proliferation at a concentration of 1 µM[3].
BJ-2302 (0.01-1 µM; 19-73 h) inhibits 5-hydroxytryptamine (5-HT)-induced proliferation, invasion, CTSS/MMP-9 expression, and Src phosphorylation in MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human triple-negative breast cancer (TNBC) cells
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Concentration:0.01, 0.1, 1 and 10 µM
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Incubation Time:18 h
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Result:Inhibited serum-induced MDA-MB-231 cell invasion in a concentration-dependent manner, with an IC50 of 0.08 µM and an IC90 of 0.71 µM.
Demonstrated stronger maximum inhibitory effect than Z-FL-COCHO or batimastat, which had IC90 values greater than 10 µM.
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Cell Line:MDA-MB-231 human TNBC cells
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Concentration:0.01, 0.1, 1 and 10 µM
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Incubation Time:1 h pre-incubation, then 72 h incubation with serum
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Result:Inhibited serum-induced MDA-MB-231 cell proliferation in a concentration-dependent manner.
Achieved complete suppression of serum-induced cell proliferation at 1 µM.
BJ-2302 (3-30 pmol/CAM; administered at cell seeding; treatment duration of 5 days) exerts concentration-dependent inhibition on tumor growth, angiogenesis and metastasis of triple-negative breast cancer in the chick embryo chorioallantoic membrane (CAM) xenograft model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude (7-8 weeks old, female, triple-negative breast cancer subcutaneous model)[3]
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Dosage:1 mg/kg
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Administration:i.p.; daily; 25 days
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Result:Significantly suppressed tumor volume and tumor weight, with greater efficacy than Z-FL-COCHO (HY-15533) (1 mg/kg) or Batimastat (HY-13564) (30 mg/kg).
Reduced in vivo bioluminescent imaging signals from tumors much lower compared to controls and other treatment groups.
Did not cause progressive body weight loss.
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Animal Model:Fertile chicken embryos (developing, triple-negative breast cancer CAM xenograft model)[3]
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Dosage:3 pmol/CAM; 30 pmol/CAM
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Administration:at cell inoculation; maintained for 5 days
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Result:Suppressed tumor growth and tumor-induced angiogenesis in a concentration-dependent manner, with greater efficacy than Z-FL-COCHO (30 pmol/CAM) or Batimastat (300 pmol/CAM).
Significantly suppressed metastasis of MDA-MB-231-luc2-tdTomato cells to the lungs, liver, and bottom CAM, as evidenced by reduced red-fluorescence-labeled cancer cells and decreased human HPRT mRNA expression in these tissues, with stronger activity than Z-FL-COCHO or batimastat.
Chemical Information
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CAS. Nr. 1631056-29-5
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Molecular Weight 178.19
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Formel C9H10N2O2
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SMILES
O=C1NC2=C(C1)C(C)=C(O)C(C)=N2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Yang SF, et al. Melatonin attenuates epidermal growth factor-induced cathepsin S expression in ARPE-19 cells: Implications for proliferative vitreoretinopathy. J Pineal Res. 2020;68(1):e12615. [Content Brief]
[2]. Liao M, et al. Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions. J Med Chem. 2021;64(5):2382-2418. [Content Brief]
[3]. Gautam J, et al. Down-regulation of cathepsin S and matrix metalloproteinase-9 via Src, a non-receptor tyrosine kinase, suppresses triple-negative breast cancer growth and metastasis. Exp Mol Med. 2018;50(9):1-14. Published 2018 Sep 5. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BJ-2302 Related Classifications
HY-182614 Related Classifications
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