JET-209 is an exceptionally potent PROTAC degrader of CBP/p300. JET-209, achieved a half-maximal degradation (DC50) value of 0.05 nM for CBP and 0.2 nM for p300 with maximum degradation (Dmax) >95% for both proteins in the RS4;11 leukemia cell line after 4 h of treatment. JET-209 achieved subnanomolar to low nanomolar DC50 values in the inhibition of cell growth in several representative acute leukemia cell lines and was much more potent than CBP/p300 bromodomain and catalytic domain inhibitors. JET-209 effectively inhibited tumor growth in xenograft tumor models at tolerated dose schedules.
MedKoo Cat#: 123937
Name: JET-209
CAS#: N/A
Chemical Formula: C46H47N9O6
Exact Mass: 821.3600
Molecular Weight: 821.94
Elemental Analysis: C, 67.22; H, 5.76; N, 15.34; O, 11.68
The following data is based on the product molecular weight 821.94 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
