dPDL1-4
dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77 μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799)).
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- Formule: C60H74BrN7O10
- Masse moléculaire:1133.17
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
dPDL1-4 (5-20 μM, 12-24 h) promotes degradation of membrane PD-L1 in an eHSP90-, ternary complex- and lysosome-dependent manner in HeLa and B16F10 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa and B16F10 cells
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Concentration:0, 1, 3, 5, 10, 20 μM
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Incubation Time:12 h
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Result:Induced dose- and time-dependent degradation of PD-L1 in HeLa cells (Dmax = 68%) and B16F10 cells (Dmax = 56%).
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Cell Line:B16F10 cells
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Concentration:5 μM
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Incubation Time:12 h
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Result:Inhibited the degradation of membrane-associated PD-L1 by BMS-8 (HY-116274) or HSP90i-Ac.
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Cell Line:HeLa cells
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Concentration:10, 20 μM
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Incubation Time:24 h
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Result:Inhibited the degradation of membrane-associated PD-L1 by Bafilomycin A1 (HY-100558) and Monensin (HY-N4302) but not by MG132 (HY-13259).
| Species | Dose | Route | AUC0-∞ | T1/2 |
|---|---|---|---|---|
| Rat[1] | 50 mg/kg | i.v. | 27866.1 μg/L·h | 1.6 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 melanoma syngeneic mouse model established by tumor-bearing mice (C57BL/6J, 6-7 weeks, female)[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection (i.p.), once every 2 days for 6 doses.
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Result:Suppressed tumor growth significantly, without causing notable weight loss.
Induced a remarkable decrease in the PD-L1 level among all the treatments.
Increased the percentage of activated cytotoxic T cells (CD8+cells).
Chemical Information
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Masse moléculaire 1133.17
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Formule C60H74BrN7O10
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SMILES
CC(C1=C(C=C(C(C2=NN=C(N2C3=CC=C(C=C3)CN4CCN(CC4)C(CCOCCOCCOCCOCCNC(C5CCCCN5CC6=CC=C(OCC7=C(C(C8=CC=CC=C8)=CC=C7)C)C(Br)=C6)=O)=O)O)=C1)O)O)C
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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)
dPDL1-4 Related Classifications
HY-174468 Related Classifications
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