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Cat. No.: HY-P11888

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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
화학식: C₉₂H₁₂₆N₂₂O₂₄S
분자량:1956.18

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

DK 221 Chemical Structure

CAS No.: 1886065-39-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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.

In Vivo

DK221 (50 mg/kg; 30 min prior to [¹⁸F]DK222 injection) specifically blocks [¹⁸F]DK222 binding to PD-L1 in MDAMB231 breast cancer xenografts, resulting in a 79% reduction in radiotracer tumor uptake at a dose of 50 mg/kg^[1].
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.

Animal Model:

NSG (5-6-wk-old, male or female, immunocompromised)^[1]
Dosage:

50 mg/kg
Administration:

30 min prior to [¹⁸F]DK222 injection
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.

Animal Model:

NSG (5-6-wk-old, male or female, immunocompromised)^[1]
Dosage:

50 mg/kg
Administration:

30 min prior to [¹⁸F]DK222 injection
Result:

Drastically reduced [¹⁸F]DK222 accumulation in LOX-IMVI tumors compared to mice not receiving DK221 (P < 0.0001).

Chemical Information

CAS No. 1886065-39-9
분자량 1956.18
화학식 C₉₂H₁₂₆N₂₂O₂₄S
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
Sequence

Cyclo(Ac-Tyr-NMeAla-Asn-Pro-His-Glu-Hyp-Trp-Ser-Trp(carboxymethyl)-NMeNle-NMeNle-Lys-Cys)-Gly-NH2
Sequence Shortening

Cyclo(Ac-Y-NMeAla-NPHEWS-Trp(carboxymethyl)-NMeNle-NMeNle-KC)-G-NH2
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Kumar D, et al. Pharmacodynamic measures within tumors expose differential activity of PD(L)-1 antibody therapeutics. Proc Natl Acad Sci U S A. 2021 Sep 14;118(37):e2107982118. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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