CADD522 is a novel small molecule inhibitor of RUNX2, downregulates RUNX2-mediated transcription of downstream target genes by inhibiting RUNX2-DNA binding, with an IC50 of 10 nM. The inhibition of the promoter-Luc activities of MMP13 in T47D-RUNX2 cells was almost completely blocked by CADD522 at 2 μM. The intraperitoneal (i.p.) administration of CADD522 into the MMTV-PyMT mice (up to 20 mg/kg) delayed tumor development and reduced tumor burden in transgenic MMTV-PyMT mice.
| Molecular Weight | 326.17 |
| Formula | C15H13Cl2NO3 |
| CAS Number | 199735-88-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage | 2-8°C, dry, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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