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PROTAC TTK degrader-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PROTAC TTK degrader-2图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

PROTACTTK degrader-2 is a potentTTK(threonine tyrosine kinase)PROTACdegrader, withDC50values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively.PROTACTTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectalcancercells[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 ofTTKprotein in a dose-dependent manner[1].

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 anIC50of 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 ofTTKprotein 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

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.