PARP1/BRD4-IN-2 (40 and 80 mg/kg; IG, for 16 days) significantly inhibits tumor growth in xenograft mice and without significant toxicities, and significantly down-regulates the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues[1].
Pharmacokinetic Parameters of PARP1/BRD4-IN-2 in Sprague-Dawley rats[1].
| IV (1 mg/kg) | PO (10 mg/kg) |
| T1/2 (h) | 3.02 ± 0.57 | 3.33 ± 0.71 |
| Cmax (ng/mL) | 258 ± 11 | 242 ± 6 |
| AUC0-t (ng/mL·h) | 629 ± 49 | 1489 ± 130 |
| AUC0-∞ (ng/mL·h) | 642 ± 36 | 1530 ± 146 |
| VZ (L/kg) | 21.1 ± 2.6 | |
| CL (mL/min/kg) | 33.7 ± 1.5 | |
| F (%) | | 23.8 ± 1.3 |
| Animal Model: | Female BALB/c nude mice (implanted subcutaneously with MDA-MB-468 tumor cells)[1] |
| Dosage: | 40 and 80 mg/kg |
| Administration: | IG, for 16 days |
| Result: | Significantly inhibited tumor growth and exhibits no significant toxicities; and significantly down-regulated the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues. |
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