Cat. No.: HY-143904

PROTAC TTK degrader-1

Name: PROTAC TTK degrader-1
Brand: MedChemExpress
SKU: HY-143904
Price: 360.00 USD
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PROTAC TTK degrader-1 is a PROTAC degrader targeting Threonine Tyrosine Kinase (TTK), with a DC₅₀ of 5.8 nM in HCT-116 cells and 1.7 nM in COLO-205 cells. PROTAC TTK degrader-1 induces the formation of a ternary complex with TTK and the CRBN E3 ubiquitin ligase, triggering proteasome-mediated degradation. PROTAC TTK degrader-1 exhibits activity against colon cancer cells and shows anti-tumor activity in a colon cancer xenograft mouse model. It can be used in colon cancer-related research.
(Pink: Mps1 Target protein ligand; Blue: Cereblon ligand (HY-W243404); Black: linker (HY-Y0925)).

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Pureté : 98.01%
CAS No.: 2953426-43-0
Formule: C₄₇H₅₃N₉O₇
Masse moléculaire:855.98

Stockage:

4°C, protect from light

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

PROTAC TTK degrader-1 Chemical Structure

CAS No.: 2953426-43-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

PROTAC TTK degrader-1 is a PROTAC degrader targeting Threonine Tyrosine Kinase (TTK), with a DC₅₀ of 5.8 nM in HCT-116 cells and 1.7 nM in COLO-205 cells. PROTAC TTK degrader-1 induces the formation of a ternary complex with TTK and the CRBN E3 ubiquitin ligase, triggering proteasome-mediated degradation. PROTAC TTK degrader-1 exhibits activity against colon cancer cells and shows anti-tumor activity in a colon cancer xenograft mouse model. It can be used in colon cancer-related research^[1]. (Pink: Mps1 Target protein ligand; Blue: Cereblon ligand (HY-W243404); Black: linker (HY-Y0925)).

IC₅₀ & Target

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

Voir tous les produits spécifiques à Isoform PROTACs :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	0.1 μM Compound: 8e	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

Anti-cancer

PROTAC TTK degrader-1 (compound 8e) potently degrades TTK protein in COLO-205 human colorectal cancer cells, with a DC₅₀ of 1.7 nM and a maximum degradation rate of 88% after 6 h of treatment; it also potently degrades TTK protein in HCT-116 human colorectal cancer cells, with a DC₅₀ of 5.8 nM and a maximum degradation rate of 80% after 6 h of treatment^[1].
PROTAC TTK degrader-1 (5-50 nM; 6 h) induces dose-dependent TTK degradation in LOVO, HCT-8 and HCT-29 human colorectal cancer cells; it also induces TTK degradation in COLO-205 human colorectal cancer cells, and this degradation effect persists for 6-8 h after compound washout^[1].
PROTAC TTK degrader-1 (5-50 nM; 6 h) induces TTK degradation in human COLO-205 colorectal cancer cells, and this degradation effect is abolished by simultaneous administration of 5 μM TTK inhibitor 6, verifying that its degradation activity relies on target protein binding^[1].
PROTAC TTK degrader-1 (5-50 nM; 1 h pretreatment followed by 6 h incubation) triggers TTK degradation in human COLO-205 colorectal cancer cells through proteasome-dependent pathways, and pre-treatment with 5 μM MG132 (HY-13259) completely abolishes this TTK degradation effect^[1].
PROTAC TTK degrader-1 (0.000508-10 μM; 96 h) potently inhibits the proliferation of human colorectal cancer cell line COLO-205, with an IC₅₀ of 0.1 μM after 96 h of treatment^[1].

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

Western Blot Analysis^[1]

Cell Line:

LOVO, HCT-8, HCT-29 human colorectal cancer cells
Concentration:

5, 50 nM
Incubation Time:

6 h
Result:

Induced 43%, 57%, 62%, and 69% TTK degradation in LOVO, HCT-116, HCT-8, and HCT-29 cells respectively at 5 nM.
Induced 85%, 78%, 90%, and 80% TTK degradation in LOVO, HCT-116, HCT-8, and HCT-29 cells respectively at 50 nM.

Western Blot Analysis^[1]

Cell Line:

COLO-205 human colorectal cancer cells
Concentration:

5 nM
Incubation Time:

6 h pretreatment, then 1, 2, 4, 8, 16, 24 h incubation after washout
Result:

Maintained obvious TTK degradation for 6-8 h after washout.
Allowed complete recovery of protein levels by 16 h post-washout.

Western Blot Analysis^[1]

Cell Line:

COLO-205 human colorectal cancer cells
Concentration:

5, 50 nM; 5 μM TTK inhibitor 6 (co-treatment)
Incubation Time:

6 h
Result:

Completely prevented TTK degradation induced by 5 nM of the compound via co-treatment with 5 μM TTK inhibitor 6.
Completely prevented TTK degradation induced by 50 nM of the compound via co-treatment with 5 μM TTK inhibitor 6.

Western Blot Analysis^[1]

Cell Line:

COLO-205 human colorectal cancer cells
Concentration:

5, 50 nM; 5 μM MG132 (pretreatment)
Incubation Time:

1 h pretreatment, then 6 h compound incubation
Result:

Completely prevented TTK degradation induced by 5 nM of the compound via pretreatment with 5 μM proteasome inhibitor MG132.
Completely prevented TTK degradation induced by 50 nM of the compound via pretreatment with 5 μM proteasome inhibitor MG132.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	T_1/2
Rat^[1]	10 mg/kg	i.p.	2235 ng/mL·h	4.3 h

In Vivo

Anti-cancer

PROTAC TTK degrader-1 (compound 8e) (10-20 mg/kg; i.p.; daily; 16 days) exhibits potent in vivo TTK degradation and a 46.0% tumor growth inhibition^[1].

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

Animal Model:

CB17-SCID (male)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; daily; 16 days
Result:

Did not show obvious tumor growth inhibition at 10 mg/kg daily.
Achieved a tumor growth inhibition (TGI) value of 46.0% at 20 mg/kg daily.
Significantly reduced TTK protein levels in tumor tissues from both dose groups compared to vehicle controls.
Did not cause significant body weight loss in treated mice.

Related Protocols :

Chemical Information

CAS No. 2953426-43-0
Appearance Solid
Masse moléculaire 855.98
Formule C₄₇H₅₃N₉O₇
Color Light yellow to yellow
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1683 mL

5.8413 mL

11.6825 mL

5 mM

0.2337 mL

1.1683 mL

2.3365 mL

10 mM

0.1168 mL

0.5841 mL

1.1683 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lu J, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. Journal of medicinal chemistry. 2022 Feb 10;65(3):2313-2328. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Voir tous les produits spécifiques à Isoform PROTACs