XYD113
XYD113 is an orally active, selective GSPT1 Molecular glue degrader. XYD113 promotes the formation of the CRBN-GSPT1 ternary complex and mediates GSPT1 degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. XYD113 downregulates genes associated with the occurrence and progression of prostate cancer (c-Myc, AR, AR-V7, KLK3, KLK2, TMPRSS2). XYD113 exhibits anticancer activity against prostate cancer. XYD113 can be used in the research of prostate cancer.
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- No. CAS: 3032314-99-8
- Fòrmula: C21H21ClN4O4
- Peso molecular:428.87
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Ver todos los productos específicos de isoformas Eukaryotic Release Factor (eRF)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
eRF3a/GSPT1 |
AR-V7 |
KLK3 |
KLK2 |
TMPRSS2 |
CRBN |
In Vitro
XYD113 (96 h) potently inhibits the proliferation of 22Rv1 cells, with an IC50 of 69 nM[1].
XYD113 (12-1000 nM; 1-12 h) induces dose- and time-dependent degradation of GSPT1 in 22Rv1 cells, with potency comparable to that of MRT-2359 (HY-153356); meanwhile, this compound shows high selectivity, as it does not degrade SALL4, IKZF1/2/3, ZFP91 or CK1α even at a concentration of 1 μM[1].
XYD113 (100-500 nM; 12 h) effectively downregulates the expression of genes critical for prostate cancer initiation and progression in 22Rv1 cells when applied at concentrations of 100 nM and 500 nM for 12 h[1].
As a molecular glue, XYD113 (0.1-100 μM; 1.5 h) promotes the formation of the CRBN-GSPT1 ternary complex in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:human prostate cancer 22Rv1 cells
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Concentration:range of concentrations
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Incubation Time:96 h
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Result:Potently inhibited 22Rv1 cell proliferation with an IC50 of 69 nM.
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Cell Line:human prostate cancer 22Rv1 cells
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Concentration:12-1000 nM (6 h incubation); 100 nM (1-12 h incubation); 1 μM (6 h incubation)
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Incubation Time:6 h (12-1000 nM, 1 μM); 1-12 h (100 nM)
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Result:Induced complete degradation of GSPT1 at 1 μM after 6 h.
Reduced GSPT1 protein levels in a dose-dependent manner across 12-1000 nM after 6 h.
Reduced GSPT1 protein levels in a time-dependent manner across 1-12 h at 100 nM.
Showed no significant degradation of off-target substrates SALL4, IKZF1, IKZF2, IKZF3, ZFP91, or CK1α even at 1 μM after 6 h.
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Cell Line:human prostate cancer 22Rv1 cells
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Concentration:100-500 nM
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Incubation Time:12 h
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Result:Significantly downregulated mRNA expression levels of c-Myc, AR, AR-V7, KLK3, KLK2, and TMPRSS2.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nude (5 weeks old)[1]
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Dosage:5 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 46%.
Showed no significant body weight loss during treatment.
Caused significant downregulation of GSPT1 protein levels in harvested tumor tissues.
Revealed no tissue abnormalities in major organs (heart, liver, spleen, lung, kidney) compared to vehicle control.
Chemical Information
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No. CAS 3032314-99-8
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Peso molecular 428.87
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Fòrmula C21H21ClN4O4
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SMILES
ClC1=CC(NC(NCC2=CC=CC(C(NC3CCC(NC3=O)=O)=O)=C2)=O)=CC=C1C
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Envío
Room temperature in continental US; may vary elsewhere.
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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)
XYD113 Related Classifications
HY-184896 Related Classifications
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Keywords
- XYD113
- 3032314-99-8
- XYD 113
- XYD-113
- Molecular Glues
- Eukaryotic Release Factor (eRF)
- c-Myc
- Androgen Receptor
- Kallikrein
- Ser/Thr Protease
- E1/E2/E3 Enzyme
- CRBN
- ubiquitin-proteasome system
- MYC-overexpressing cancer cells
- MOLM-16 cells
- BALB/c-nude mice
- GSPT1
- G1 to S phase transition 1
- MV4-11 cells
- 22Rv1 cells
- prostate cancer
- Inhibitor
- inhibitor
- inhibit