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PROTAC TTK degrader-2

Catalog No. T81374   CAS 2953426-48-5

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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PROTAC TTK degrader-2 Chemical Structure
PROTAC TTK degrader-2, CAS 2953426-48-5
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

PROTAC TTK degrader-2 2953426-48-5 PROTAC PROTACs inhibitor inhibit

 

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