SY-5102

• Description :

  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].

• CAS Number :

  [2365230-48-2]

• UNSPSC :

  12352005

• Target :

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

• Related Pathways :

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

• Field of Research :

  Cancer

• Smiles :

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

• Molecular Formula :

  C22H22F3N7O

• Molecular Weight :

  457.45

• References & Citations :

  [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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  CDK2; CDK7