PROTAC ROR1 degrader-1
PROTAC ROR1 degrader-1 is a ROR1 PROTAC degrader with DC50 values of 40.88 nM (NCI-H23), 69.0 nM (NCI-H460), 83.35 nM (NCI-H1299) and 42.07 nM (NCI-H1975), respectively. PROTAC ROR1 degrader-1 inhibits the proliferation of lung cancer cells and induces apoptosis. PROTAC ROR1 degrader-1 can be used in research related to non-small cell lung cancer.
(Pink: ROR1 ligand (HY-170996); Blue: VHL ligand (HY-125845); Black: linker (HY-W014787)).
For research use only. We do not sell to patients.
- Formula: C55H74BrN11O5S
- Molecular Weight:1081.22
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
PROTAC ROR1 degrader-1 (Compound 11d) (0.1-1 μM; 24 h) potently degrades ROR1 protein in NCI-H23 non-small cell lung cancer cells. After 24 h of treatment, the degradation rate reaches 93.0% at 0.1 μM and 99.7% at 1 μM[1].
PROTAC ROR1 degrader-1 (1 μM; 4-24 h) induces time-dependent degradation of ROR1 in NCI-H23 non-small cell lung cancer cells. Degradation is detectable at 1 μM within 4 h and reaches the maximum level at 24 h[1].
PROTAC ROR1 degrader-1 (72 h) potently inhibits the proliferation of NCI-H23, NCI-H1975, NCI-H1299 and NCI-H460 non-small cell lung cancer cells, with IC50 values of 0.036 μM, 0.063 μM, 0.164 μM and 0.085 μM respectively after 72 hours of treatment[1].
PROTAC ROR1 degrader-1 (0.1-1.0 μM; 24 h) induces dose-dependent apoptosis in NCI-H23 non-small cell lung cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H23 non-small cell lung cancer cells
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Concentration:0.1 μM, 1 μM
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Incubation Time:24 h
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Result:Achieved ROR1 degradation rates of 93.0% at 0.1 μM and 99.7% at 1 μM after 24-hour treatment.
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Cell Line:NCI-H23 non-small cell lung cancer cells
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Concentration:1 μM
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Incubation Time:4 h, 24 h
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Result:Induced ROR1 degradation starting at 4 hours post-treatment, reaching maximal degradation at 24 hours.
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Cell Line:NCI-H23 non-small cell lung cancer cells
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Concentration:0.1 μM, 0.3 μM, 1.0 μM
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Incubation Time:24 h
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Result:Induced dose-dependent apoptosis, with early apoptosis rates of 29.9% (0.1 μM), 46.5% (0.3 μM), and 46.9% (1.0 μM), and corresponding late apoptosis rates of 6.5% (0.1 μM), 20.1% (0.3 μM), and 22.1% (1.0 μM).
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Cell Line:NCI-H23 non-small cell lung cancer cells
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Concentration:0.1 μM, 1 μM
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Incubation Time:10 h
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Result:Cleaved PARP at 0.1 μM, while completely activated PARP at 1 μM.
Chemical Information
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Molecular Weight 1081.22
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Formula C55H74BrN11O5S
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SMILES
O=C([C@H]1N(C([C@@H](NC(CCCCCCCCC(N2CCN(C3=CC=C(C4=NC5=C(NC6CCN(CC)CC6)C(Br)=CN=C5N4)C=C3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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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)
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