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.
For research use only. We do not sell to patients.
- CAS No.: 1886065-39-9
- Formula: C92H126N22O24S
- Molecular Weight:1956.18
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Storage:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
DK 221 (1 μM; 30 min) specifically blocks [18F]DK222 binding to PD-L1 in PD-L1-positive CHO-hPD-L1, LOX-IMVI, MDAMB231, and SUM149 cells, with >90% reduction in radioactivity uptake[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
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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Molecular Weight 1956.18
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Formula 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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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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