SY-5102
SY-5102 is a potent, selective, and orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd value of 0.03 nM. SY-5102 occupies the ATP-binding pocket of CDK7 via non-covalent binding to inhibit CDK7 activity, and downregulates its phosphorylation of cyclin CDK and RNA polymerase II. SY-5102 inhibits cancer cell proliferation, and induces tumor growth inhibition and regression. SY-5102 can be used in research related to triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2365230-48-2
- Formula: C22H22F3N7O
- Molecular Weight:457.45
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CDK7 0.03 nM (Kd) |
CDK2 189 nM (IC50) |
CDK9 90 nM (IC50) |
CDK12 75 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC70 | EC50 |
9 nM
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Antiproliferative activity against human HCC70 triple-negative breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 assay.
Antiproliferative activity against human HCC70 triple-negative breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 assay.
|
34726887 |
In Vitro
SY-5102 (1 μM) exhibits exceptionally high kinome selectivity in the SelectScreen biochemical kinase assay involving 485 kinases[1].
SY-5102 (3 × 10-10 M-1 × 10-5 M) exerts the strongest inhibitory effect on the target CDK7/CycH/MAT1 complex (IC50 = 2.36 nM), and exhibits a significant activity window against other family members such as CDK2/9/12, with IC50 values of 189 nM, 90 nM, and 75 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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)[1]
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Dosage:2.5 mg/kg; 4 mg/kg
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Administration:p.o.; twice daily; 21 days
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Result:Exhibited dose-dependent tumor growth inhibition.
Significantly reduced tumor volumes compared to vehicle controls at 2.5 mg/kg twice daily.
Induced tumor regression at 4 mg/kg twice daily, with tumor volumes remaining low through the post-treatment observation period.
Achieved statistically significant antitumor effect.
- Western Blot
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 2365230-48-2
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Molecular Weight 457.45
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Formula C22H22F3N7O
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SMILES
FC(F)(C1=CN=C(N[C@H]2CCCNC2)N=C1C3=CNC4=NC(C5=C(C)ON=C5C)=CC=C34)F
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Shipping
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SY-5102 Related Classifications
HY-180355 Related Classifications
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