SY-5102

SY-5102 is a potent, selective and orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd of 0.03 nM. SY-5102 shows anti-proliferative activity against HCC70 cells with an EC50 of 9 nM. SY-5102 can inhibit CDK7-mediated CAK function (downregulate CDK2 Thr160 phosphorylation) and TFIIH transcription function (downregulate RNA polymerase II Ser5 phosphorylation) . SY-5102 can induce G2/M cell cycle arrest, downregulate the expression of the oncogene c-Myc, and ultimately trigger cancer cell apoptosis. SY-5102 can be used for the research of triple-negative breast cancer (TNBC) [1].

2365230-48-2

12352005

Apoptosis; CDK; c-Myc; Ser/Thr Kinase

Apoptosis; Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Cancer

FC(F)(C1=CN=C(N[C@H]2CCCNC2)N=C1C3=CNC4=NC(C5=C(C)ON=C5C)=CC=C34)F

C22H22F3N7O

457.45

[1]Marineau JJ, et al. Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J Med Chem. 2022 Jan 27;65 (2) :1458-1480.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-180355/

Reference compound1

No Development Reported

CDK2; CDK7