PROTAC TTK degrader-2

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PROTAC TTK degrader-2 

PROTAC TTK degrader-2 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 3.1 和 12.4 nM。PROTAC TTK degrader-2 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

PROTAC TTK degrader-2

PROTAC TTK degrader-2 Chemical Structure

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生物活性

PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 3.1 nM (TTK) in COLO-205, 12.4 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-2 (compound 8j) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-2 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.2 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.

体内研究
(In Vivo)

PROTAC TTK degrader-2 (8j) (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-2 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-2 in male SD rats[1].

8j
AUC (ng/mL*h) 2333
T1/2 (h) 3.2

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SD rats (, three animals per group)[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (xenograft mouse model of COLO-205 cells)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 36.7% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.

分子量

884.03

Formula

C49H57N9O7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lu J, Huang Y, Huang J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022;65(3):2313-2328.

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