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PROTAC TTK degrader-2
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Catalog No. T81374Cas No. 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].
PROTAC TTK degrader-2
😃Good
Catalog No. T81374Cas No. 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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Product Introduction
Bioactivity
Chemical Properties
| 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 from 0 to 10 μM over 96 hours, inhibits cancer cell proliferation [1]. |
| In vivo | PROTAC TTK degrader-2 (8j) administered intraperitoneally at 10 mg/kg exhibits satisfactory pharmacokinetic profiles [1]. Daily intraperitoneal dosing of 10 or 20 mg/kg for 16 days significantly reduces TTK protein levels and suppresses tumor growth [1]. Pharmacokinetic parameters for PROTAC TTK degrader-2 were established in male SD rats [1]. |
| Molecular Weight | 884.03 |
| Formula | C49H57N9O7 |
| Cas No. | 2953426-48-5 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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