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  4. PROTAC TTK degrader-1

PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.

For research use only. We do not sell to patients.

PROTAC TTK degrader-1 Chemical Structure

PROTAC TTK degrader-1 Chemical Structure

CAS No. : 2953426-43-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

PROTAC TTK degrader-1 Related Antibodies

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Description

PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 1.7 nM (TTK) in COLO-205, 5.8 nM (TTK) in HCT-116[1]
In Vitro

PROTAC TTK degrader-1 (compound 8e) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-1 (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-1 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 0.1 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-1 (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-1 (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-1 in male SD rats[1].

8e
AUC (ng/mL*h) 2235
T1/2 (h) 4.3

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

Animal Model: Male SD rats[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 (bearing COLO-205 tumor xenografts)[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 46.0% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.
Molecular Weight

855.98

Formula

C47H53N9O7
CAS No.
Appearance

Solid

SMILES

O=C1N(C2=NC(NC3=C(C=C(C=C3)N4CCN(CC4)C(CCCC#CC5=CC=C6C(N(CC6=C5)C7C(NC(CC7)=O)=O)=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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (116.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1683 mL 5.8413 mL 11.6825 mL
5 mM 0.2337 mL 1.1683 mL 2.3365 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1683 mL 5.8413 mL 11.6825 mL 29.2063 mL
5 mM 0.2337 mL 1.1683 mL 2.3365 mL 5.8413 mL
10 mM 0.1168 mL 0.5841 mL 1.1683 mL 2.9206 mL
15 mM 0.0779 mL 0.3894 mL 0.7788 mL 1.9471 mL
20 mM 0.0584 mL 0.2921 mL 0.5841 mL 1.4603 mL
25 mM 0.0467 mL 0.2337 mL 0.4673 mL 1.1683 mL
30 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9735 mL
40 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
50 mM 0.0234 mL 0.1168 mL 0.2337 mL 0.5841 mL
60 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 mL
80 mM 0.0146 mL 0.0730 mL 0.1460 mL 0.3651 mL
100 mM 0.0117 mL 0.0584 mL 0.1168 mL 0.2921 mL
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PROTAC TTK degrader-1 Related Classifications

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-12953426-43-0PROTAC TTK degrader1PROTAC TTK degrader 1PROTACsCOLO-205 cancer cellsHuman colorectal cancerPharmacokinetics propertiesAnticancerInhibitorinhibitorinhibit

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