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).
For research use only. We do not sell to patients.
- Formula: C43H51FN6O5
- Molecular Weight:750.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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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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Molecular Weight 750.90
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Formula 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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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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