Multi-kinase-IN-8
Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C25H21N7O5S
- 分子量:531.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
COX-2 0.05 μM (IC50) |
COX-1 12.6 μM (IC50) |
VEGFR2 0.12 nM (IC50) |
体外実験
Multi-kinase-IN-8 (Compound 5j) inhibits the proliferation of cancer cell lines, with IC50 of 1.30 μM (MB 231 cell), 9.53 μM (MCF-7 cell), 2.07 μM (A549 cell), and 2.28 μM (Caco-2 cell), respectively[1].
Multi-kinase-IN-8 (2.07 μM, 72 h) inhibits VEGFR-2 in Caco-2 cells[1].
Multi-kinase-IN-8 (24 h and 48 h) induces cell cycle arrest at the G1 phase in Caco-2 cells[1].
Multi-kinase-IN-8 (24 h and 48 h) induces cell death by triggering apoptosis in Caco-2 cells[1].
Multi-kinase-IN-8 (24 h and 48 h) downregulates HIF-1α mRNA expression, and reduces PGE2, total VEGFR-2, p-VEGFR-2 production in MDA-MB 231[1].
Multi-kinase-IN-8 has selective targeting potential towards the tumor-associated CA isoforms, particularly hCA IX, due to its interaction with the catalytic zinc binding site[1].
Multi-kinase-IN-8 reduces expression levels of the initiator caspase-9 and mitochondrial apoptotic markers Bcl-2 and Bax in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Caco-2 cells
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Concentration:2.07 μM
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Incubation Time:72 h
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Result:Suppressed Caco-2 cell migration with 56.29 % wound closure.
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Cell Line:Caco-2 cells
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Concentration:
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Incubation Time:24 h and 48 h
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Result:Increased of % Caco-2 cells in G0 / G1 phase from 62.07 % in the control to 86.36 %.
Reduced nearly 3-fold in % Caco-2 cells in both S phase and G2 / M phase.
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Cell Line:Caco-2 cells
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Concentration:
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Incubation Time:24 h and 48 h
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Result:Increased 42 fold in total apoptosis.
Increased the ratio of annexin V-FITC positive early apoptotic cells from 0.54 % to 20.26 %, whilst the percentage of late apoptotic cells rose from 0.22 % to 11 %.
Resulted in a combined percentage of early and late apoptotic cells that significantly exceeded the percentage of necrotic cells. (Early apoptotic cells is 20.26%, late apoptotic cells is 11.32%, necrotic cells is 3.61%).
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cyclosporine (HY-100563A)-preconditioned (30 mg/kg/day, for 1 week) male BALB/c mice and then injected with MDA-MB 231 cells (1 × 106 per mouse)[1].
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Dosage:50 mg/kg
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Administration:s.c., daily, five consecutive days, dissolved in 100 μL of DMSO (HY-Y0320C) /PBS (HY-K3005) (1:20, v/v).
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Result:Reduced tumor size.
Induced 92.3 % tumor regression.
Had no significant changes in body weight were observed during the treatment course, indicating a satisfactory safety profile.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Mitochondrial membrane-potential fluorescent assay
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
化学情報
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分子量 531.54
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分子式 C25H21N7O5S
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SMILES
O=S(C1=CC=C(N2N=NC(COC3=CC=C(/C=N/N=C4C(NC5=C\4C=C(OC)C=C5)=O)C=C3)=C2)C=C1)(N)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Multi-kinase-IN-8 関連分類
HY-179439 関連分類
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