BJ-2302 

BJ-2302 is a Src kinase inhibitor with an IC₅₀ of 3.23 μM, and inhibits cathepsin S (CTSS) activity^[1][2].BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression^[2][3].BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth^[1][2][3].BJ-2302 does not induce cytotoxicity in normal breast epithelial cells^[3].BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer^[1][2][3].

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.

BJ-2302 (1 mg/kg; i.p.; once daily; for 25 consecutive days) exerts a significant inhibitory effect on the growth of triple-negative breast tumors in BALB/C nude mice, without inducing progressive body weight loss^[3].
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.

178.19

C₉H₁₀N₂O₂

1631056-29-5

O=C1NC2=C(C1)C(C)=C(O)C(C)=N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.

  [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.