2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. 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.

XYD224

XYD224 Chemical Structure

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XYD224 Related Antibodies

Top Publications Citing Use of Products

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Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

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Description

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)[1]. (Pink: BRD9 ligand (HY-184211); Blue: Cereblon ligand (HY-179307); Black: linker).

IC50 & Target[1]

BRD9

7.3 nM (DC50)

Cereblon

 

In Vitro

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.

XYD224 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MV4-11, MOLM-16, MOLM-13 and Kasumi-1 cells
Concentration: 0.0001, 0.01, 1, 100 μM
Incubation Time: 72 h (MOLM-16, MOLM-13 and Kasumi-1) and 120 h (MV4-11)
Result: Had strong anti-proliferative activity against multiple AML cell lines.
Parmacokinetics
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
In Vivo

XYD224 (10-20 mg/kg; i.p.; daily; 14 days) achieves tumor growth inhibition rates of 70% and 79%, respectively, with a favorable safety profile in the MV4-11 AML xenograft mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID (male, 4 weeks old, subcutaneous xenograft model via injection of 3 × 106 MV4-11 cells)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 14 days
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.
Molecular Weight

750.90

Formula

C43H51FN6O5
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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XYD224 Related Classifications

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XYD224XYD 224XYD-224PROTACsEpigenetic Reader DomainBRD9proteasomeMV4-11 AML xenograft mouse modelxenograft modelsCRBNacute myeloid leukemia cellsInhibitorinhibitorinhibit

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