Syk-IN-16
Syk-IN-16 is a spleen tyrosine kinase (SYK) inhibitor with an IC50 of 16.0 nM. Syk-IN-16 exerts antiproliferative effects, induces cell apoptosis, inhibits cell migration and increases DNA damage in cancer cells. Syk-IN-16 suppresses tumor growth in xenograft models without obvious toxicity. Syk-IN-16 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3102293-90-0
- Formula: C28H32N6O4
- Molecular Weight:516.59
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
Description
Syk-IN-16 is a spleen tyrosine kinase (SYK) inhibitor with an IC50 of 16.0 nM. Syk-IN-16 exerts antiproliferative effects, induces cell apoptosis, inhibits cell migration and increases DNA damage in cancer cells. Syk-IN-16 suppresses tumor growth in xenograft models without obvious toxicity. Syk-IN-16 can be used for the research of triple-negative breast cancer[1].
In Vitro
Anti-cancerCell ProliferationApoptosisEMT / Metastasis
Anti-cancer
Cell Proliferation
Anti-cancer
Cell Proliferation
Syk-IN-16 (2.5-10 μM) potently inhibits the colony-forming ability of MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner[1].
Anti-cancer
Cell Proliferation
Syk-IN-16 (2.5-10 μM; 24 h) reduces DNA synthesis in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating that it inhibits cell proliferation[1].
Anti-cancer
Apoptosis
Syk-IN-16 (2.5-10 μM; 24 h) induces apoptosis in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells in a dose-dependent manner[1].
Anti-cancer
Apoptosis
Treatment with Syk-IN-16 (2.5-10 μM; 24 h) induces morphological changes characteristic of apoptosis in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells[1].
Anti-cancer
Apoptosis
Syk-IN-16 (2.5-10 μM; 24 h) regulates the expression of apoptosis-related proteins in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells, and enhances pro-apoptotic characteristics after 24 h of treatment[1].
Anti-cancer
EMT / Metastasis
Syk-IN-16 (2.5-10 μM; 24 h) inhibits the migratory capacity of MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells[1].
Anti-cancer
EMT / Metastasis
Syk-IN-16 (2.5-10 μM) inhibits the migratory capacity of MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells[1].
Anti-cancer
EMT / Metastasis
Syk-IN-16 (2.5-10 μM) regulates the expression of migration-related proteins in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells, downregulating MMP-2 and upregulating E-cadherin[1].
Anti-cancer
EMT / Metastasis
Syk-IN-16 (2.5-10 μM; 24 h) reduces the expression of MMP-2 and upregulates the expression of E-cadherin in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
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Cell Line:MDA-MB-231, BT-549 TNBC cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Significantly reduced the population of DNA-synthesizing cells in both MDA-MB-231 and BT-549 cell lines in a concentration-dependent manner.
Apoptosis Analysis[1]
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Cell Line:MDA-MB-231, BT-549 TNBC cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Resulted in a dose-dependent increase in the percentage of apoptotic cells in both MDA-MB-231 and BT-549 cell lines.\nInduced characteristic apoptotic morphology, including nuclear condensation and fragmentation, in both MDA-MB-231 and BT-549 cell lines.
Western Blot Analysis[1]
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Cell Line:MDA-MB-231, BT-549 TNBC cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Upregulated the expression of pro-apoptotic proteins Bax, Cleaved-Caspase 3, and Cleaved-PARP in both cell lines.
Downregulated the expression of anti-apoptotic protein Bcl-2 in both cell lines.
Cell Migration Assay[1]
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Cell Line:MDA-MB-231, BT-549 TNBC cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Significantly impeded wound closure in both MDA-MB-231 and BT-549 cell lines compared to the control group.
Immunofluorescence[1]
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Cell Line:MDA-MB-231, BT-549 TNBC cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Reduced the intensity of MMP-2 staining in both MDA-MB-231 and BT-549 cell lines.
Increased the intensity of E-cadherin staining in both MDA-MB-231 and BT-549 cell lines.
Parmacokinetics
In Vivo
Anti-cancerApoptosisCell Cycle Regulation
Anti-cancer
Apoptosis
Cell Cycle Regulation
Syk-IN-16 (Compound 5i) (10-20 mg/kg; i.p.; daily; 14 days) dose-dependently suppresses triple-negative breast cancer tumor growth in MDA-MB-231 xenografts[1].
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 (female, 6−8 weeks old, 16−17 g, subcutaneously inoculated with MDA-MB-231 cells)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Showed progressive disease in all tumors at 10 mg/kg dose.
Showed progressive disease in 58% of tumors, stable disease in 14% of tumors, and partial response in 28% of tumors at 20 mg/kg dose.
Reduced tumor weight and volume significantly compared to control, with a clear dose-dependent response.
Reduced Ki67 and Bcl-2 expression in tumor tissue.
Increased Cleaved Caspase-3 expression in tumor tissue.
Downregulated MMP-2 expression in tumor tissue.
Caused no significant body weight changes or histopathological abnormalities in major organs.
Related Protocols :
- Scratch/Wound-Healing Migration Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- 3D Collagen/Hydrogel Matrix Migration Assay
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Genotoxicity/Mutagenicity Study
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 3102293-90-0
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Molecular Weight 516.59
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Formula C28H32N6O4
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SMILES
O=C(NC1=CC=C2N=C(NC2=C1)NC3=CC=C(C=C3)N4CCN(CC4)C)C5=CC(OC)=C(C(OC)=C5)OC
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Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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