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.
For research use only. We do not sell to patients.
- CAS No.: 1049691-47-5
- Formula: C17H20ClN3O2S
- Molecular Weight:365.88
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Storage:
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]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vivo
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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CAS No. 1049691-47-5
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Molecular Weight 365.88
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Formula C17H20ClN3O2S
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SMILES
COC(C(OC)=C1)=CC=C1CCNC2=C3C=C(C)SC3=NC=N2.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NR2F2-IN-1 Related Classifications
HY-156190 Related Classifications
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