Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [1].
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Description | PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [1]. |
In vitro | PROTAC TTK degrader-2 (compound 8j) at concentrations ranging from 0 to 10 μM over a period of 96 hours impedes the proliferation of cancer cells [1]. |
In vivo | PROTAC TTK degrader-2 (8j) administered intraperitoneally at a single dose of 10 mg/kg showcases satisfactory pharmacokinetic profiles [1]. Additionally, with a daily intraperitoneal dose of 10 or 20 mg/kg over 16 days, it markedly diminishes TTK protein levels and demonstrates significant tumor growth suppression [1]. The pharmacokinetic parameters for PROTAC TTK degrader-2 have been established in male SD rats [1]. |
Molecular Weight | 884.03 |
Formula | C49H57N9O7 |
CAS No. | 2953426-48-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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PROTAC TTK degrader-2 2953426-48-5 PROTAC PROTACs inhibitor inhibit