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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2365230-48-2
- Fòrmula: C22H22F3N7O
- Peso molecular:457.45
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
CDK7 0.03 nM (Kd) |
CDK2 189 nM (IC50) |
CDK9 90 nM (IC50) |
CDK12 75 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCC70 | EC50 |
9 nM
|
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 |
SY-5102 (maximum concentration of 20 nM; 70 seconds of exposure, 300 seconds of dissociation) exhibits high-affinity binding activity to the purified CDK7/Cyclin H dimer complex, with a Kd value of 0.03 nM[1].
SY-5102 (1 μM) exhibits exceptionally high kinome selectivity in the SelectScreen biochemical kinase assay involving 485 kinases[1].
SY-5102 (0.3 μM-10 nM) 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].
SY-5102 (72 h) significantly inhibits cell proliferation in HCC70 cells, with an IC50 value of 9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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)[1]
-
Dosage:2.5 mg/kg; 4 mg/kg
-
Administration:p.o.; twice daily; 21 days
-
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.
Chemical Information
-
No. CAS 2365230-48-2
-
Peso molecular 457.45
-
Fòrmula C22H22F3N7O
-
SMILES
FC(F)(C1=CN=C(N[C@H]2CCCNC2)N=C1C3=CNC4=NC(C5=C(C)ON=C5C)=CC=C34)F
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SY-5102 Related Classifications
HY-180355 Related Classifications
Powered by Bioz