dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC) which exhibits significant and selective degradation of BRD4 BD1 but is inactive on BRD4 BD2. dBET57 mediates recruitment to the CRL4CRBN E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1.
| Molecular Weight | 699.18 |
| Formula | C34H31ClN8O5S |
| CAS Number | 1883863-52-2 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage | 2-8°C, protect from light |
| 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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DGY-09-192 is a bivalent degrader that couples the pan-FGFR inhibitor BGJ398 to the CRL2VHL E3 ligase-recruiting ligand, which induces degradation of FGFR1/2 and largely avoids degradation of FGFR3/4.DGY-09-192 exhibits a nanomolar DC50 against both wild-type FGFR2 and several FGFR2 fusions. In addition, DGY-09-192 has antiproliferative activity in gastric and cholangiocarcinoma cells. |
| BTX-6654
BTX-6654 is a targeted and specific cerebellar-based bifunctional SOS1 PROTAC degrader.BTX-6654 reduces the downstream signaling markers pERK and pS6 and displays antiproliferative activity in a wide range of KRAS-mutant cells. |
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