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Cat. No.: HY-182614

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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 No.: 1631056-29-5
화학식: C₉H₁₀N₂O₂
분자량:178.19

보관:

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

BJ-2302 Chemical Structure

CAS No.: 1631056-29-5

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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].

All Src Isoforms :

All Cathepsin Isoforms :

All PI3K Isoforms :

All Akt Isoforms :

All Ras Isoforms :

All Raf Isoforms :

All ERK Isoforms :

All MMP Isoforms :

In Vitro

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.

Cell Invasion Assay^[3]

Cell Line:

MDA-MB-231 human triple-negative breast cancer (TNBC) cells
Concentration:

0.01, 0.1, 1 and 10 µM
Incubation Time:

18 h
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.

Cell Proliferation Assay^[3]

Cell Line:

MDA-MB-231 human TNBC cells
Concentration:

0.01, 0.1, 1 and 10 µM
Incubation Time:

1 h pre-incubation, then 72 h incubation with serum
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.

In Vivo

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.

Animal Model:

BALB/C nude (7-8 weeks old, female, triple-negative breast cancer subcutaneous model)^[3]
Dosage:

1 mg/kg
Administration:

i.p.; daily; 25 days
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.

Animal Model:

Fertile chicken embryos (developing, triple-negative breast cancer CAM xenograft model)^[3]
Dosage:

3 pmol/CAM; 30 pmol/CAM
Administration:

at cell inoculation; maintained for 5 days
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

CAS No. 1631056-29-5
분자량 178.19
화학식 C₉H₁₀N₂O₂
SMILES

O=C1NC2=C(C1)C(C)=C(O)C(C)=N2
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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수량:
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Species:
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수량:

BJ-2302

All Src Isoforms

All Cathepsin Isoforms

All PI3K Isoforms

All Akt Isoforms

All Ras Isoforms

All Raf Isoforms

All ERK Isoforms

All MMP Isoforms