Molecular Formula | C18H14BrNO5S2 |
Molar Mass | 468.34 |
Density | 1.79±0.1 g/cm3(Predicted) |
Boling Point | 661.2±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 28 mg/mL |
pKa | 2.41±0.30(Predicted) |
Storage Condition | -20℃ |
In vitro study | UMI-77 effectively interferes with BL-Noxa and cell Mcl-1 interactions, as well as Mcl-1/Bax protein-protein interactions. UMI-77 inhibited the growth of pancreatic cancer cells with IC50 values of 3.4,4.4,12.5,16.1, 5.5, and μm for BxPC-3,Panc-1,MiaPaCa-2,AsPC-1, and Capan-2 cells, respectively. UMI-77 induces apoptosis of pancreatic cancer cells by activating the intrinsic apoptotic pathway and/or Bax conformational changes. |
In vivo study | In a BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg I. v.) exhibited a single dose of anti-tumor activity without damaging normal tissue at all. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.135 ml | 10.676 ml | 21.352 ml |
5 mM | 0.427 ml | 2.135 ml | 4.27 ml |
10 mM | 0.214 ml | 1.068 ml | 2.135 ml |
5 mM | 0.043 ml | 0.214 ml | 0.427 ml |
biological activity | UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing higher selectivity than other members of the Bcl-2 family. |
in vitro studies | UMI-77 effectively interfere with the interaction between BL-Noxa and cell Mcl-1, as well as Mcl-1/Bax protein-protein interaction. UMI-77 inhibit the growth of pancreatic cancer cells, the IC50 for BxPC-3,Panc-1,MiaPaCa-2,AsPC-1 and Capan-2 cells is 3.4,4.4,12.5,16.1, and 5.5 μM respectively. UMI-77 induce apoptosis of pancreatic cancer cells by activating the inherent apoptosis pathway and/or Bax conformational changes. |
in vivo study | in BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg I. v.) showed single dose anti-tumor activity without damaging normal tissues at all. |