Art. -Nr.: HY-161409

SC912

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SC912 is an AR-V7 inhibitor (IC₅₀ = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis.

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Reinheit: 99.13%
Formel: C₂₂H₁₃Cl₂F₃N₄O₂
Molecular Weight:493.27

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SC912 Chemical Structure

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

SC912 (0.1-10 μM; 24 h) effectively inhibits AR activation in PC3 Cells. No inhibition of GR and PR (AR IC₅₀ = 0.57 μM)^[1].
SC912 (0.03-100 μM; 1 h) binding to AR-FL and AR-V7 is attenuated in 293 T cells deleted for AR-NTD amino acids 507-531. Amino acids 507-531 are essential for the antagonistic activity^[1].
SC912 (2 μM; 24 h) strongly represses the transcription of AR-regulated genes (PSA, FKBP5, TMPRSS2) that are uniquely regulated by AR-V7 in the LNCaP95 cell model, suggesting effective repression of AR-V7-mediated transcriptional activity^[1].
SC912 (1 μM; 24 h) leads to G1 phase blockade and causes apoptosis in LNCaP, VCaP and 22Rv1 cells^[1].
SC912 (3 μM; 5 h) significantly reduces the intranuclear accumulation of AR-FL and AR-V7 in LNCaP and LNCaP-AR-V7 cells, suggesting that is able to effectively block the nuclear localization of AR-V7. SC912 also significantly reducs the binding of AR proteins to the chromatin^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

LNCaP, VCaP, 22Rv1cell, PC3
Concentration:

1 μM
Incubation Time:

24 h
Result:

SC912 led to significant PARP cleavage in LNCaP, VCaP, and 22Rv1 cells, indicating effective induction of apoptosis. Flow cytometry analysis showed an increase in the percentage of apoptotic cells in LNCaP, VCaP, and 22Rv1 cell lines with SC912. This further supported the finding that SC912 induces apoptosis effectively in AR-positive cells.

Real Time qPCR^[1]

Cell Line:

LNCaP, VCaP, 22Rv1
Concentration:

0, 0.1, 0.3, 1, 3 μM
Incubation Time:

24 h
Result:

SC912-dependent dose (0.33 μM) impaired the transcription of AR-regulated genes (PSA, FKBP5 and TMPRSS2) in these prostate cancer cell lines.This indicates effective inhibition of AR signaling by SC912. The inhibition of gene expression was dose-dependent.

Cell Cycle Analysis^[1]

Cell Line:

LNCaP, VCaP, 22Rv1cell, PC3
Concentration:

3 μM
Incubation Time:

48 h
Result:

Induced a significant G1/S phase arrest in the treated cells. This effect was dose-dependent, with higher concentrations of SC912 leading to a more pronounced accumulation of cells in the G1 phase, suggesting a blockade in the transition from G1 to S phase.

In Vivo

SC912 (60 mg/kg; i.p.;5 times days for 3 weeks) halts the growth of VCaP tumors effectively. No noticeable loss in body weight of the mice, indicating good tolerability at the administered dose^[1].
SC912 (90 mg/kg; i.p.; 5 days a week for 3 weeks) alleviates tumor progression even in this highly castration-resistant 22Rv1 model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD-SCID mice implanted with VCaP cells ^[1]
Dosage:

60 mg/kg, five times a week for 3 weeks
Administration:

i.p.
Result:

SC912 was found to effectively repress tumor growth in the xenograft models. This was evidenced by a marked reduction in tumor size in mice treated with SC912 compared to those treated with vehicle controls. The serum levels of human PSA, a marker of AR activity, were considerably lower , indicating effective inhibition of AR signaling.

Animal Model:

mice implanted with 22Rv1 cells ^[1]
Dosage:

90 mg/kg, five times a week for 3 weeks
Administration:

i.p.
Result:

SC912 markedly mitigated tumor progression in this highly castration-resistant 22Rv1 model. The growth rate of tumors was significantly reduced in the SC912-treated group compared to the vehicle-treated controls. Reduction in tumor size was associated with a significant decrease in AR-driven gene expression within the tumors, highlighting SC912’s capability to interrupt AR-V7-mediated signaling pathways even under high AR-V7 expressing conditions.

Chemical Information

Appearance Solid
Molecular Weight 493.27
Formel C₂₂H₁₃Cl₂F₃N₄O₂
Color White to off-white
SMILES

N#CC1=CC=CC(NC(NC2=CC=C(C(F)(F)F)C=C2NC(C3=CC(Cl)=CC(Cl)=C3)=O)=O)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (202.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0273 mL

10.1364 mL

20.2729 mL

5 mM

0.4055 mL

2.0273 mL

4.0546 mL

10 mM

0.2027 mL

1.0136 mL

2.0273 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Qianhui Y et al. SC912 inhibits AR-V7 activity in castration-resistant prostate cancer by targeting the androgen receptor N-terminal domain Oncogene. 2024 Mar [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.0273 mL	10.1364 mL	20.2729 mL	50.6822 mL
	5 mM	0.4055 mL	2.0273 mL	4.0546 mL	10.1364 mL
	10 mM	0.2027 mL	1.0136 mL	2.0273 mL	5.0682 mL
	15 mM	0.1352 mL	0.6758 mL	1.3515 mL	3.3788 mL
	20 mM	0.1014 mL	0.5068 mL	1.0136 mL	2.5341 mL
	25 mM	0.0811 mL	0.4055 mL	0.8109 mL	2.0273 mL
	30 mM	0.0676 mL	0.3379 mL	0.6758 mL	1.6894 mL
	40 mM	0.0507 mL	0.2534 mL	0.5068 mL	1.2671 mL
	50 mM	0.0405 mL	0.2027 mL	0.4055 mL	1.0136 mL
	60 mM	0.0338 mL	0.1689 mL	0.3379 mL	0.8447 mL
	80 mM	0.0253 mL	0.1267 mL	0.2534 mL	0.6335 mL
	100 mM	0.0203 mL	0.1014 mL	0.2027 mL	0.5068 mL

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SC912

Apoptosis Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SC912

Apoptosis Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SC912 Related Classifications

Art. -Nr.: HY-161409