PROTAC tubulin-Degrader-1
PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)).
(Pink: Microtubule/Tubulin ligand (HY-N2146); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Formula: C35H35N3O10
- Molecular Weight:657.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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Cereblon |
α-tubulin 296 nM (DC50, A549 cells) |
α-tubulin 32 nM (DC50, A549/Taxol cells) |
β-tubulin 856 nM (DC50, A549 cells) |
β-tubulin 972 nM (DC50, A549/Taxol cells) |
β3-tubulin 251 nM (DC50, A549 cells) |
β3-tubulin 5 nM (DC50, A549/Taxol cells) |
PROTAC tubulin-Degrader-1 (Compound W13) (4-21 nM, 72 h) exhibits potent antiproliferative activity against multiple human tumor cell lines (MCF-7, A549, HepG2, MGC-803, HeLa, U937), with IC50 values ranging from 0.004 μM to 0.021 μM[1].
PROTAC tubulin-Degrader-1 (0-1.25 μM, 48 h) effectively degrades α-tubulin (DC50 = 296 nM in A549, DC50 = 32 nM in A549/Taxol), β-tubulin (DC50 = 856 nM in A549, DC50 = 972 nM in A549/Taxol) and potently degrades β3-tubulin (DC50 = 251 nM in A549, DC50 = 5 nM in A549/Taxol) in A549 and A549/Taxol cells[1].
PROTAC tubulin-Degrader-1 (0.25 μM, 24-48 h) induces tubulin degradation via the ubiquitin-proteasome system (UPS)[1].
PROTAC tubulin-Degrader-1 (2-50 nM, 24-48 h) induces G2/M phase arrest and promotes apoptosis in A549 and A549/Taxol cells in a dose-dependent manner[1].
PROTAC tubulin-Degrader-1 (2-50 nM, 14 days) inhibits colony formation of A549 and A549/Taxol cells in a dose-dependent manner[1].
PROTAC tubulin-Degrader-1 (2.5-10 nM, 6-8 h) strongly inhibits tube formation of human umbilical vein endothelial cells (HUVECs) on Matrigel, reducing the number of nodes, master junctions, segments length, total branching length and meshes in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and A549/Taxol cells
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Concentration:2, 10, 50 nM
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Incubation Time:24 h
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Result:Induced G2/M phase arrest in A549 and A549/Taxol cells in a dose-dependent manner.
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Cell Line:A549 and A549/Taxol cells
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Concentration:2, 10, 50 nM
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Incubation Time:48 h
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Result:Induced apoptosis in A549 and A549/Taxol cells in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 cells or A549/Taxol cells (1 × 107) were subcutaneously implanted into the right hind flanks of 5-6-week-old male nude mice[1]
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Dosage:15 mg/kg
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Administration:i.p., once every two days, 23 days
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Result:Achieved tumor growth inhibition (TGI) rate of 34.1% in A549 xenograft mice and a higher tumor growth inhibition (TGI) rate of 65.8% in A549/Taxol (Taxol-resistant) xenograft mice.
Showed no significant changes in body weight.
Chemical Information
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Molecular Weight 657.67
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Formula C35H35N3O10
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SMILES
COC1=C(OC)C(OC)=CC(/C=C\C2=CC=C(OC)C(OC(CCCN3C(CCC(N4C(C(C(N)=CC=C5)=C5C4=O)=O)C3=O)=O)=O)=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)