2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. XYD270

XYD270 is an orally active BRD9 PROTAC degrader. XYD270 inhibits the proliferation of cancer cells. XYD270 suppresses tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia.
(Pink: BRD9 ligand (HY-182084); Blue: Cereblon ligand (HY-150799); Black: linker (HY-W262798)).

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XYD270

XYD270 화학구조

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XYD270 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • 순도&문서

  • References

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제품 설명

XYD270 is an orally active BRD9 PROTAC degrader. XYD270 inhibits the proliferation of cancer cells. XYD270 suppresses tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia[1]. (Pink: BRD9 ligand (HY-182084); Blue: Cereblon ligand (HY-150799); Black: linker (HY-W262798)).

IC50 & Target[1]

Cereblon

 

BRD9

 

In Vitro

XYD270 (Compound 32) (0-500 nM, 24 h) potently and selectively degrades BRD9 in HS-SY-II and MV4;11 cells, with a DC50 of 0.082 nM and 3.9 nM, and a Dmax of 96% and 90%, respectively[1].
XYD270 (0.0001-100 μM; 96 h) potently inhibits the proliferation of HS-SY-II synovial sarcoma cells (IC50 = 1.65 μM) and MV4;11 acute myeloid leukemia cells (IC50 = 0.05 μM), and suppresses the long-term colony formation of HS-SY-II cells[1].

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

XYD270 Related Antibodies

Western Blot Analysis[1]

Cell Line: HS-SY-II synovial sarcoma cells
Concentration: 0, 0.03, 0.16, 0.8, 4, 20, 100, 500 nM
Incubation Time: 24 h
Result: Induced potent, concentration-dependent BRD9 degradation with a DC50 of 0.082 nM and a maximal degradation (Dₘₐₓ) of 96%.
Achieved significant BRD9 degradation (89%) within 0.5 h of treatment with 10 nM.
Did not reduce protein levels of BRD4, BRD7, or CRBN neo-substrates (GSPT1, IKZF1, CK1α).
Confirmed significant BRD9 downregulation with no significant changes in homologous bromodomain proteins or CRBN neo-substrates via label-free quantitative proteomic profiling.

Western Blot Analysis[1]

Cell Line: MV4;11 acute myeloid leukemia cells
Concentration: 0, 0.03, 0.16, 0.8, 4, 20, 100, 500 nM
Incubation Time: 24 h
Result: Induced concentration-dependent BRD9 degradation with a DC50 of 3.9 nM and a Dₘₐₓ of 90%.
Did not induce degradation of CRBN neo-substrates (GSPT1, IKZF1, CK1α).
Confirmed significant BRD9 downregulation with no significant changes in homologous bromodomain proteins or CRBN neo-substrates via label-free quantitative proteomic profiling.

Cell Proliferation Assay[1]

Cell Line: HS-SY-II synovial sarcoma cells, MV4;11 acute myeloid leukemia cells
Concentration: 0.0001, 0.01, 1, 100 μM
Incubation Time: 96 h
Result: Inhibited HS-SY-II cell proliferation with an IC50 of 1.65 μM, and MV4;11 cell proliferation with an IC50 of 0.05 μM.
Inhibited HS-SY-II colony formation in a concentration-dependent manner with superior efficacy compared to dBRD9.
In Vivo

XYD270 (10 mg/kg; p.o.; once daily; 28 days) achieves 54% tumor growth inhibition in the MV4;11 AML xenograft model of BALB/c-Nude mice, with no significant body weight loss observed[1].

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

Animal Model: BALB/c-Nude (male, 5 weeks old, subcutaneous inoculation with MV4;11 cells)[1]
Dosage: 10 mg/kg
Administration: p.o.; once daily; 28 days
Result: Achieved a tumor growth inhibition (TGI) rate of 54%.
Showed no significant reduction in body weight.
분자량

692.85

화학식

C40H48N6O5
SMILES

CC(C1=CC(C2=CC(OC)=C(CN3CCC(CN4CCN(C5=CC=C(NC6CCC(NC6=O)=O)C=C5)CC4)CC3)C(OC)=C2)=C7C=CC=CN71)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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XYD270 Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

XYD270XYD 270XYD-270PROTACsEpigenetic Reader DomainBRD9 PROTAC degraderHS-SY-II cellsMV4;11 cellsBALB/c-Nude micesynovial sarcomaacute myeloid leukemiaInhibitorinhibitorinhibit

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상품명:
XYD270
Cat. No.:
HY-182082
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