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).
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- Formule: C43H51FN6O5
- Masse moléculaire:750.90
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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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.
Chemical Information
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Masse moléculaire 750.90
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Formule 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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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)
XYD224 Related Classifications
HY-184210 Related Classifications
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