DK 221
DK 221 is a PD-L1 blocker with an IC50 of 24.5 nM for inhibiting the binding of PD-L1 to PD-1. DK 221 reduces the uptake of [18F]DK222 in PD-L1-positive tumor cells and mouse xenografts. DK 221 is applicable to research related to triple-negative breast cancer and melanoma.
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- CAS No.: 1886065-39-9
- Formule: C92H126N22O24S
- Masse moléculaire:1956.18
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
DK221 (50 mg/kg; 30 min prior to [18F]DK222 injection) specifically blocks [18F]DK222 binding to PD-L1 in LOX-IMVI melanoma xenografts, resulting in significantly reduced radiotracer tumor uptake at a dose of 50 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (5-6-wk-old, male or female, immunocompromised)[1]
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Dosage:50 mg/kg
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Administration:30 min prior to [18F]DK222 injection
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Result:Reduced [18F]DK222 uptake in MDAMB231 tumors by 79% compared to mice not receiving DK221 (P < 0.0001).
Reduced [18F]DK222 uptake in MDAMB231 tumors in a dose-dependent manner, but not in low PD-L1-expressing SUM149 tumors or other tissues.
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Animal Model:NSG (5-6-wk-old, male or female, immunocompromised)[1]
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Dosage:50 mg/kg
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Administration:30 min prior to [18F]DK222 injection
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Result:Drastically reduced [18F]DK222 accumulation in LOX-IMVI tumors compared to mice not receiving DK221 (P < 0.0001).
Chemical Information
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CAS No. 1886065-39-9
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Masse moléculaire 1956.18
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Formule C92H126N22O24S
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SMILES
CN([C@H](C(N[C@H](C(NCC(N)=O)=O)CSCC(N[C@H]1CC2=CC=C(O)C=C2)=O)=O)CCCCN)C([C@@H](N(C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]3C[C@@H](O)CN3C([C@@H](NC([C@@H](NC([C@@H]4CCCN4C([C@@H](NC([C@@H](N(C1=O)C)C)=O)CC(N)=O)=O)=O)CC5=CNC=N5)=O)CCC(O)=O)=O)=O)CC6=CNC7=CC=CC=C76)=O)CO)=O)CC(C8=CC=CC=C89)=CN9CC(O)=O)=O)CCCC)=O)C)CCCC)=O
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Sequence
Cyclo(Ac-Tyr-NMeAla-Asn-Pro-His-Glu-Hyp-Trp-Ser-Trp(carboxymethyl)-NMeNle-NMeNle-Lys-Cys)-Gly-NH2
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Sequence Shortening
Cyclo(Ac-Y-NMeAla-NPHEWS-Trp(carboxymethyl)-NMeNle-NMeNle-KC)-G-NH2
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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)
DK 221 Related Classifications
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