SKLB-03220

• Description :

  SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer[1].

• UNSPSC :

  12352005

• Target :

  Apoptosis; Histone Methyltransferase

• Related Pathways :

  Apoptosis; Epigenetics

• Field of Research :

  Cancer

• Smiles :

  O=C(NC1=CC=C(C)C(C2=CC(N(C3CCOCC3)CC)=C(C)C(C(NCC4=C(C)C=C(C)NC4=O)=O)=C2)=C1)C=C

• Molecular Formula :

  C33H40N4O4

• Molecular Weight :

  556.70

• References & Citations :

  [1]Zhang Q, et al. Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer. J Med Chem. 2023 Feb 9;66 (3) :1725-1741.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  EZH2

• CAS Number :

  [2852050-29-2]