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)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C40H48N6O5
- Peso molecular:692.85
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
More
Actividad biológica
Descripciòn
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.
-
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.
-
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 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
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.
Chemical Information
-
Peso molecular 692.85
-
Fòrmula 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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XYD270 Related Classifications
HY-182082 Related Classifications
Powered by Bioz