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  4. PROTAC TTK degrader-2

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.

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PROTAC TTK degrader-2 Chemical Structure

PROTAC TTK degrader-2 Chemical Structure

CAS No. : 2953426-48-5

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PROTAC TTK degrader-2 Related Antibodies

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Description

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]
Cellular Effect
Cell Line Type Value Description References
COLO 205 IC50
0.2 μM
Compound: 8j
Antiproliferative against human COLO 205 cells assessed as cell viability after 4 days by CCK-8 assay
Antiproliferative against human COLO 205 cells assessed as cell viability after 4 days by CCK-8 assay
[PMID: 35084180]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC TTK degrader-2 Related Antibodies

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.
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

MedChemExpress (MCE) 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.
Molecular Weight

884.03

Formula

C49H57N9O7
CAS No.
SMILES

O=C1N(C2=NC(NC3=C(C=C(C=C3)N4CCN(CC4)C(CCCCCC#CC5=CC6=C(C=C5)CN(C7C(NC(CC7)=O)=O)C6=O)=O)OC)=NC=C2C(C)=C1)[C@@H]8CC[C@@H](CC8)NC(CC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC TTK degrader-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC TTK degrader-22953426-48-5PROTAC TTK degrader2PROTAC TTK degrader 2PROTACsCOLO-205 cancer cellsHuman colorectal cancerPharmacokinetics propertiesAnticancerInhibitorinhibitorinhibit

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