NR2F2-IN-1 free base
Based on 1 Customer Validation
NR2F2-IN-1 (free base) is a COUP-TFII (orphan nuclear receptor NR2F2) inhibitor with antitumor activity against prostate cancer. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators including FOXA1. NR2F2-IN-1 (free base) can be used for the research of prostate cancer.
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 452087-38-6
- Formula: C17H19N3O2S
- Molecular Weight:329.42
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
NR2F2-IN-1 free base (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 free base (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 free base (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 free base (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.
-
Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, subcutaneous xenograft of 10×106 LNCaP cells mixed with Matrigel)[1]
-
Dosage:2.6 mg/kg
-
Administration:i.p.; daily
-
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.
-
Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, subcutaneous xenograft of 2×106 PC3 cells mixed with Matrigel)[1]
-
Dosage:2.6 mg/kg
-
Administration:i.p.; daily
-
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.
-
Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, castrated, subcutaneous xenograft of 10×106 LNCaP-abl cells mixed with Matrigel)[1]
-
Dosage:2.6 mg/kg
-
Administration:i.p.; daily
-
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.
-
Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, subcutaneous xenograft of 4×106 22Rv1 cells mixed with Matrigel)[1]
-
Dosage:2.6 mg/kg
-
Administration:i.p.; daily
-
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.
-
Animal Model:Nu/J (male, 6 weeks old, homozygous for Foxn1nu, patient-derived xenograft (PDX) model)[1]
-
Dosage:2.6 mg/kg
-
Administration:i.p.; daily
-
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
-
CAS No. 452087-38-6
-
Appearance Solid
-
Molecular Weight 329.42
-
Formula C17H19N3O2S
-
Color Light yellow to yellow
-
SMILES
COC(C(OC)=C1)=CC=C1CCNC2=C3C=C(C)SC3=NC=N2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (379.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (278 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0356 mL | 15.1782 mL | 30.3564 mL | 75.8910 mL |
| 5 mM | 0.6071 mL | 3.0356 mL | 6.0713 mL | 15.1782 mL | |
| 10 mM | 0.3036 mL | 1.5178 mL | 3.0356 mL | 7.5891 mL | |
| 15 mM | 0.2024 mL | 1.0119 mL | 2.0238 mL | 5.0594 mL | |
| 20 mM | 0.1518 mL | 0.7589 mL | 1.5178 mL | 3.7945 mL | |
| 25 mM | 0.1214 mL | 0.6071 mL | 1.2143 mL | 3.0356 mL | |
| 30 mM | 0.1012 mL | 0.5059 mL | 1.0119 mL | 2.5297 mL | |
| 40 mM | 0.0759 mL | 0.3795 mL | 0.7589 mL | 1.8973 mL | |
| 50 mM | 0.0607 mL | 0.3036 mL | 0.6071 mL | 1.5178 mL | |
| 60 mM | 0.0506 mL | 0.2530 mL | 0.5059 mL | 1.2648 mL | |
| 80 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9486 mL | |
| 100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.7589 mL |
NR2F2-IN-1 free base Related Classifications
HY-156190A Related Classifications
Powered by Bioz