| Identification | Back Directory | [Name]
2,6-Piperidinedione, 3-[5-[3-[4-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl][1,4'-bipiperidin]-1'-yl]-1-propyn-1-yl]-1,3-dihydro-1-oxo-2H-isoindol-2-yl]- | [CAS]
2801715-13-7 | [Synonyms]
2,6-Piperidinedione, 3-[5-[3-[4-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl][1,4'-bipiperidin]-1'-yl]-1-propyn-1-yl]-1,3-dihydro-1-oxo-2H-isoindol-2-yl]- | [Molecular Formula]
C43H43N9O4 | [MOL File]
2801715-13-7.mol | [Molecular Weight]
749.86 |
| Hazard Information | Back Directory | [Uses]
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth[1]. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice[1].
| PO (100 mg/kg) | IV (2 mg/kg) | | Tmax (h) | 1.00 | | | T1/2 (h) | 8.3 | 3.7 | | Cmax (ng/mL) | 3089 | | | AUC0-t (ng/mL·h) | 16,894 | 2827 | | AUC0-∞ (ng/mL·h) | 17,070 | 2845 | | VdSS (L/kg) | | 3.1 | | CL (mL/min/kg) | | 11.7 | | MRT (h) | | 4.5 | | F (%) | 12 | |
| Animal Model: | OCI-ly10 xenograft mouse model[1] | | Dosage: | 10 and 30 mg/kg | | Administration: | PO, bid, for 17 days | | Result: | Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively. |
| [References]
[1] Zhang J, et al. Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. J Med Chem. 2022 Jun 7. DOI:10.1021/acs.jmedchem.2c00324 |
|
|