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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1886065-39-9
分子式: C₉₂H₁₂₆N₂₂O₂₄S
分子量:1956.18

保管条件:

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

DK 221 構造式

CAS 番号: 1886065-39-9

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Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

体外実験

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.

体内実験

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).

化学情報

CAS 番号 1886065-39-9
分子量 1956.18
分子式 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
配列

Cyclo(Ac-Tyr-NMeAla-Asn-Pro-His-Glu-Hyp-Trp-Ser-Trp(carboxymethyl)-NMeNle-NMeNle-Lys-Cys)-Gly-NH2
シーケンスの短縮

Cyclo(Ac-Y-NMeAla-NPHEWS-Trp(carboxymethyl)-NMeNle-NMeNle-KC)-G-NH2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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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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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