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Cat. No.: HY-184655

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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

Storage:

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

Syk-IN-16 Chemical Structure

CAS No.: 3102293-90-0

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Fluorescent Dye

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

In Vitro

Syk-IN-16 (Compound 5i) (24-72 h) inhibits the viability of MDA-MB-231, BT-549 and MCF-7 breast cancer cells in a dose-dependent manner, with 72 h IC₅₀ values ranging from 0.35, 0.72 to 1.64 μM, respectively^[1].
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].
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].
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].
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].
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].
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].
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].
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].
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]

Cell Line:

MDA-MB-231, BT-549 TNBC cells
Concentration:

2.5, 5 and 10 μM
Incubation Time:

24 h
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]

Cell Line:

MDA-MB-231, BT-549 TNBC cells
Concentration:

2.5, 5 and 10 μM
Incubation Time:

24 h
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]

Cell Line:

MDA-MB-231, BT-549 TNBC cells
Concentration:

2.5, 5 and 10 μM
Incubation Time:

24 h
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]

Cell Line:

MDA-MB-231, BT-549 TNBC cells
Concentration:

2.5, 5 and 10 μM
Incubation Time:

24 h
Result:

Significantly impeded wound closure in both MDA-MB-231 and BT-549 cell lines compared to the control group.

Immunofluorescence^[1]

Cell Line:

MDA-MB-231, BT-549 TNBC cells
Concentration:

2.5, 5 and 10 μM
Incubation Time:

24 h
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

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	V_ss	V_z	CL
Mice^[1]	1.0 mg/kg	i.v.	3.32 h	0.083 h	811.22 ng/mL	291.74 ng·h/mL	298.69 ng·h/mL	4256.25 mL/kg	15405.97 mL/kg	564.66 mL/min/kg
Mice^[1]	10.0 mg/kg	p.o.	1.18 h	0.5 h	4.56 ng/mL	3.43 ng·h/mL	9.95 ng·h/mL	/	/	/

In Vivo

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.

Animal Model:

BALB/c nude (female, 6−8 weeks old, 16−17 g, subcutaneously inoculated with MDA-MB-231 cells)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; daily; 14 days
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.

Chemical Information

CAS No. 3102293-90-0
Molecular Weight 516.59
Formula C₂₈H₃₂N₆O₄
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Li Z, et al. Integrating Machine Learning and Structure-Guided Discovery of a Novel Type II SYK Inhibitor for Treating Triple-Negative Breast Cancer. Journal of medicinal chemistry. 2026 Jun 17. [Content Brief]

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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.

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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Syk-IN-16

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Syk-IN-16 Related Classifications

HY-184655 Related Classifications