XYD224
XYD224 is a selective BRD9 PROTAC degrader with a DC50 of 7.3 nM. XYD224 inhibits the proliferation of acute myeloid leukemia cells. XYD224 suppresses tumor growth in xenograft models. XYD224 is applicable for the research of acute myeloid leukemia (AML).
(Pink: BRD9 ligand (HY-184211); Blue: Cereblon ligand (HY-179307); Black: linker).
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。
- 分子式: C43H51FN6O5
- 分子量:750.90
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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BRD9 7.3 nM (DC50) |
Cereblon |
XYD224 (0.0001-100 μM; 72-120 h) exhibits potent antiproliferative activity against multiple AML cell lines, with IC50 values of 33 nM, 0.15 μM, 0.52 μM and 0.37 μM against MV4-11, MOLM-16, MOLM-13 and Kasumi-1, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11, MOLM-16, MOLM-13 and Kasumi-1 cells
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Concentration:0.0001, 0.01, 1, 100 μM
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Incubation Time:72 h (MOLM-16, MOLM-13 and Kasumi-1) and 120 h (MV4-11)
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Result:Had strong anti-proliferative activity against multiple AML cell lines.
| Species | Dose | Route | Vz | CL | T1/2 (Elimination) |
|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 148680 mL/kg | 8816 mL/h/kg | 12.03 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (male, 4 weeks old, subcutaneous xenograft model via injection of 3 × 106 MV4-11 cells)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 70% at 10 mg/kg.
Achieved a TGI rate of 79% at 20 mg/kg.
Significantly reduced BRD9 protein levels in tumor tissues at both doses.
Caused no significant reduction in body weight.
Maintained serum levels of AST, CREA, and UREA within normal physiological ranges.
Caused no obvious histopathological changes in heart, liver, spleen, lung, or kidney tissues.
化学情報
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分子量 750.90
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分子式 C43H51FN6O5
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SMILES
O=C(CCC1NC2=CC=C(C(F)=C2)N3CC4(C3)CCN(CC4)CC5CCN(CC5)CC6=C(OC)C=C(C=C6OC)C7=C8N(C(C(C)=O)=C7)C=CC=C8)NC1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
XYD224 関連分類
HY-184210 関連分類
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