NR2F2-IN-1
NR2F2-IN-1 is a COUP-TFII (orphan nuclear receptor NR2F2) inhibitor with antitumor activity against prostate cancer. NR2F2-IN-1 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators including FOXA1. NR2F2-IN-1 can be used for the research of prostate cancer.
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- No. CAS: 1049691-47-5
- Fòrmula: C17H20ClN3O2S
- Peso molecular:365.88
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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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Actividad biológica
NR2F2-IN-1 (2.6 mg/kg; i.p.; daily) inhibits PC3 xenograft tumor growth in mice, reducing tumor volume and weight by ~37% and ~70% respectively[1].
NR2F2-IN-1 (2.6 mg/kg; i.p.; daily) potently inhibits castration-resistant LNCaP-abl xenograft tumor growth in mice, reducing tumor volume and weight by ~71% and ~87% respectively[1].
NR2F2-IN-1 (2.6 mg/kg; i.p.; daily) inhibits 22Rv1 xenograft tumor growth in mice, reducing tumor volume and weight by ~50% and ~60% respectively[1].
NR2F2-IN-1 (2.6 mg/kg; i.p.; daily) potently inhibits prostate cancer PDX tumor growth in mice, reducing tumor volume and weight by ~71% and ~70% respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, subcutaneous xenograft of 10×106 LNCaP cells mixed with Matrigel)[1]
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Dosage:2.6 mg/kg
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Administration:i.p.; daily
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Result:Reduced mean tumor volume to ~0.3 cm3 and mean tumor weight to ~0.2 g at week 5, corresponding to ~62% and ~83% reductions respectively.
Reduced Ki67-positive cells from ~45% to ~15%.
Reduced vessel density (via CD31 staining) from ~30 to ~10.
Reduced levels of COUP-TFII target genes FOXM1 and CDK1 in tumor tissue.
Increased levels of p21 in tumor tissue.
Caused no apparent body weight loss in treated mice.
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Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, subcutaneous xenograft of 2×106 PC3 cells mixed with Matrigel)[1]
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Dosage:2.6 mg/kg
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Administration:i.p.; daily
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Result:Reduced mean tumor volume to ~0.5 cm3 and mean tumor weight to ~0.3 g at week 5, corresponding to ~37% and ~70% reductions respectively.
Caused no apparent body weight loss in treated mice.
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Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, castrated, subcutaneous xenograft of 10×106 LNCaP-abl cells mixed with Matrigel)[1]
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Dosage:2.6 mg/kg
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Administration:i.p.; daily
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Result:Reduced mean tumor volume to ~0.2 cm3 and mean tumor weight to ~0.1 g at week 5, corresponding to ~71% and ~87% reductions respectively.
Caused no apparent body weight loss in treated mice.
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Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, subcutaneous xenograft of 4×106 22Rv1 cells mixed with Matrigel)[1]
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Dosage:2.6 mg/kg
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Administration:i.p.; daily
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Result:Reduced mean tumor volume to ~0.6 cm3 and mean tumor weight to ~0.6 g at week 5, corresponding to ~50% and ~60% reductions respectively.
Caused no apparent body weight loss in treated mice.
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Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, patient-derived xenograft (PDX) model)[1]
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Dosage:2.6 mg/kg
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Administration:i.p.; daily
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Result:Reduced mean tumor volume to ~0.2 cm3 and mean tumor weight to ~0.3 g at week 6, corresponding to ~71% and ~70% reductions respectively.
Caused no apparent body weight loss in treated mice.
Chemical Information
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No. CAS 1049691-47-5
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Peso molecular 365.88
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Fòrmula C17H20ClN3O2S
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SMILES
COC(C(OC)=C1)=CC=C1CCNC2=C3C=C(C)SC3=NC=N2.Cl
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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)
NR2F2-IN-1 Related Classifications
HY-156190 Related Classifications
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