PROTAC TTK degrader-2
PROTAC TTK degrader-2 is a threonine tyrosine kinase (TTK) PROTAC degrader with a DC50 of 3.1 nM in COLO-205 cells. PROTAC TTK degrader-2 induces proteasome-mediated degradation of TTK. It inhibits the proliferation of colorectal cancer cells. In colorectal cancer xenograft mouse models, PROTAC TTK degrader-2 mediates target degradation and exerts anticancer activity. PROTAC TTK degrader-2 can be used in colorectal cancer-related research.
(Pink: Mps1 Target protein ligand; Blue: Cereblon ligand (HY-W243404); Black: linker (HY-69220)).
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- CAS No.: 2953426-48-5
- Formule: C49H57N9O7
- Masse moléculaire:884.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
DC50: 3.1 nM (TTK) in COLO-205, 12.4 nM (TTK) in HCT-116[1]
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Cell Line
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Type | Value | Description | References |
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| COLO 205 | IC50 |
0.2 μM
Compound: 8j
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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
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[PMID: 35084180] |
PROTAC TTK degrader-2 (compound 8j) potently degrades TTK protein in human colorectal cancer cell line COLO-205, with a DC50 of 3.1 nM and a maximum degradation rate of 82% after 6 h of treatment; it also degrades TTK protein in human colorectal cancer cell line HCT-116, with a DC50 of 12.4 nM and a maximum degradation rate of 77% after 6 h of treatment[1].
PROTAC TTK degrader-2 (5-50 nM; 6 h) induces dose-dependent TTK degradation in LOVO, HCT-8, HCT-29 and COLO-205 human colorectal cancer cells; it induces TTK degradation in the human colorectal cancer cell line COLO-205, and this degradation persists for 6-8 h after compound washout[1].
PROTAC TTK degrader-2 (5-50 nM; 6 h) induces TTK degradation in human colorectal cancer cell line COLO-205 via a proteasome-dependent and TTK binding-required mechanism[1].
PROTAC TTK degrader-2 (0.000508-10 μM; 96 h) potently inhibits the proliferation of human colorectal cancer cell line COLO-205, with an IC50 of 0.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LOVO, HCT-8, HCT-29 human colorectal cancer cells
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Concentration:5, 50 nM
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Incubation Time:6 h
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Result:Induced 59% degradation in LOVO cells, 35% degradation in HCT-116 cells, 81% degradation in HCT-8 cells, 79% degradation in HCT-29 cells, and 66% degradation in COLO-205 cells at 5 nM.
Induced 82% degradation in LOVO cells, 75% degradation in HCT-116 cells, 82% degradation in HCT-8 cells, 79% degradation in HCT-29 cells, and 81% degradation in COLO-205 cells at 50 nM.
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Cell Line:COLO-205 human colorectal cancer cells
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Concentration:5 nM
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Incubation Time:6 h; assessed at 0, 1, 2, 4, 8, 16, and 24 h after washout
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Result:Maintained obvious TTK degradation for 6-8 h after washout.
Allowed full TTK protein level recovery by 16 h post-washout.
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Cell Line:COLO-205 human colorectal cancer cells
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Concentration:5, 50 nM; 5 μM MG132 (HY-13259) (pretreatment)
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Incubation Time:6 h; 1 h (MG132 pretreatment)
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Result:Had induced TTK degradation completely blocked by pretreatment with 5 μM MG132.
| Species | Dose | Route | AUC0-∞ | T1/2 |
|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 2333 ng/mL·h | 3.2 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17-SCID (male)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 16 days
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Result:Did not show obvious tumor growth inhibition at 10 mg/kg daily.
Achieved a tumor growth inhibition (TGI) value of 36.7% at 20 mg/kg daily.
Significantly reduced TTK protein levels in tumor tissues from both dose groups compared to vehicle controls.
Caused no significant body weight loss in treated mice.
Chemical Information
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CAS No. 2953426-48-5
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Masse moléculaire 884.03
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Formule C49H57N9O7
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- PROTAC TTK degrader-2
- 2953426-48-5
- PROTAC TTK degrader2
- PROTAC TTK degrader 2
- PROTACs
- Mps1
- LOVO human colorectal cancer cells
- proteasome
- colorectal cancer cells
- HCT-116 human colorectal cancer cells
- HCT-8 human colorectal cancer cells
- HCT-29 human colorectal cancer cells
- COLO-205 human colorectal cancer cells
- threonine tyrosine kinase
- TTK
- colorectal cancer xenograft mouse model
- Inhibitor
- inhibitor
- inhibit