Molecular Weight |
506.56 |
Formula |
C29H26N6O3 |
CAS No. |
2758117-74-5 |
SMILES |
O=C(C1=CC=CC2=C1NC(CN3C(N(C)C4=CC=C(C5=C(C)ON=C5C)C=C4C3C6=CC=CC=C6)=O)=N2)N |
Shipping |
Room temperature in continental US; may vary elsewhere. |
Storage |
Please store the product under the recommended conditions in the Certificate of Analysis. |
In Vitro |
PARP1/BRD4-IN-1 (compound III-7) (0-2 μM; 3-7 days) has potent inhibition of the growth of cancer cell lines. PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) can significantly inhibit the expression of PARP1 and BRD4 at 2 μM in SW1990 cells. PARP1/BRD4-IN-1 (1, 2 μM; 4 days) arrests the cell cycle at G0/G1 and G2/M phase in SW1990 cells. PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) has the potent efficacy on the apoptosis of SW1990 cells at 2 μM. PARP1/BRD4-IN-1 (1, 2 μM; 4 days) regulates the expression of HEXIM1, c-Myc, FOXO1, MDC1 and TOPBP1 to enhance the inhibition of DNA repair in SW1990 cells. |
In Vivo |
PARP1/BRD4-IN-1 (30mg/kg; intraperitoneal injection for 28 days) can significantly inhibit the tumor size and weight, and does not cause significant damage of the kidney, lung, spleen, liver and heart in mice. |