Art. -Nr.: HY-164373

SC428

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SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1.

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Reinheit: 98.0%
CAS. Nr.: 1898232-70-6
Formel: C₁₅H₁₀F₃N₃OS
Molecular Weight:337.32

Speicherung:

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

SC428 Chemical Structure

CAS. Nr.: 1898232-70-6

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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

SC428 (10 nM- 1 μM, 48 h), which inhibits AR-V7 (IC₅₀is 0.42 μM) and ARv567es (IC₅₀ is 1.31 μM) activity in 293T (PSA-Luc)^[1].
SC428 (5 μM, 5 h) reverses DHT-induced thermal stabilization of AR-FL (EC₅₀ is 0.31 μM) in LNCaP (CETSA), inhibits ligand-induced activation of AR in a concentration-dependent manner and is an antagonist of the F887 L mutant^[1].
SC428 (1, 2.5 and 5 μM, 30 min) inhibits the proliferation of LNCaP (IC₅₀is 1.39 μM), VCaP (IC₅₀ is 1.01 μM), 22RV1 (IC₅₀ is 1.13 μM) AR-positive cell line. The ability of anti-proliferation is weak in AR-negative cell line PC3 (IC₅₀ is 6.49 μM)^[1].
SC428 (5 μM, 5 h) attenuates transcription of AR-regulated genes in LNCaP-AR cells (ChIP experiments) , blocks AR-FL chromatin binding (confocal imaging experiments) , and reduces nuclear translocation^[1].
SC428 (2.5, 5 μmol/L, 24 h) inhibits AR signaling in prostate cancer cells that overexpress AR-V7^[1].
SC428 (0.5, 1, 2.5 and 5 μM, 24 h) has inhibitory effects on both LNCaP-ARV7 and LNCaP- ^wt cells (Enzalutamide (HY-70002)-resistant), inhibiting PSA and UBE2C at both protein and mRNA levels (WB and qPCR) ^[1].
SC428 (5 μM, 5 h) disrupts AR-V7 dimer (immunoprecipitation assay) and nuclear localization (confocal imaging technique) in 22RV1 cells^[1].

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

Real Time qPCR^[1]

Cell Line:

LNCaP-AR
Concentration:

5 μmol/L
Incubation Time:

24 h
Result:

Inhibited AR-FL transcription significantly and rogen-mediated mRNA expression.

Real Time qPCR^[1]

Cell Line:

22Rv1
Concentration:

2.5 and 5 μmol/L
Incubation Time:

24 h
Result:

2.5 mmol/L SC428 reduced AR-regulated gene mRNA to 50% of controls, whereas 5 mmol/L SC428 further reduced it to 10% to 30% of controls. AR-V7-dependent Ar signaling was blocked in 22Rv1 cells.

Real Time qPCR^[1]

Cell Line:

LNCaP-AR-V7
Concentration:

0.5, 1, 2.5 and 5 μmol/L
Incubation Time:

24 h
Result:

Inhibited the expression of PSA gene in LNCaP-AR-V7 cells and significantly decreased the mRNA level of AR-V7 specific gene UBE2C.

Western Blot Analysis^[1]

Cell Line:

LNCaP-AR-V7
Concentration:

0.5, 1, 2.5 and 5 μmol/L
Incubation Time:

24 h
Result:

Inhibited PSA-Luc with equal potency in LNCaP-AR-V7 and LNCaP-ARWT cells.

Western Blot Analysis^[1]

Cell Line:

LNCaP-AR-V7，22Rv1
Concentration:

5 μmol/L
Incubation Time:

5 h
Result:

Reduced AR-V7 homodimer.

Cell Proliferation Assay^[1]

Cell Line:

LNCaP, VCaP, 22Rv1, PC3
Concentration:

1, 2.5 and 5 μmol/L
Incubation Time:

30 min
Result:

Inhibited the proliferation of three AR-positive cell lines, and the anti-proliferation effect of SC428 on the AR-negative cell line PC3 was 6-fold lower than that on the AR-positive cell line.

Cell Proliferation Assay^[1]

Cell Line:

LNCaP-AR
Concentration:

0.1 μM - 10 μM
Incubation Time:

30 h
Result:

Overcame the ENZ-resistant AR signaling and cell proliferation driven by AR-V7.

In Vivo

SC428 (60 mg/kg; intraperitoneal injection; once daily; 18 days) inhibited AR-V7 tumor growth by inducing tumor cell apoptosis in mice^[1].
SC428 (90 mg/kg; intraperitoneal injection; five times a week; 3 weeks) inhibited the growth of AR-V7 in mice^[1].

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

Animal Model:

22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice^[1].
Dosage:

60 mg/kg
Administration:

Intraperitoneal injection (i.p.) ; daily route 5 days a week; 3 weeks
Result:

Reduced the tumor growth by 50% , the mice did not lose weight, and the tumor PSA was reduced to undetectable levels.

Animal Model:

22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice. Male Nu/Nu mice were surgically castrated when the implanted 22Rv1 cells achieved an average tumor size of 200 mm³^[1].
Dosage:

90 mg/kg
Administration:

Intraperitoneal injection (i.p.); daily route 5 days a week; 3 weeks
Result:

Inhibited the growth of prostate cancer with high expression of AR-V7.Good drug tolerance, no significant weight loss.

Chemical Information

CAS. Nr. 1898232-70-6
Appearance Solid
Molecular Weight 337.32
Formel C₁₅H₁₀F₃N₃OS
Color White to yellow
SMILES

N#CC1=CC=C(NC(N/C=C/C2=CC=CS2)=O)C=C1C(F)(F)F
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 (296.45 mM; ultrasonic and warming and heat to 60°C; 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

2.9645 mL

14.8227 mL

29.6454 mL

5 mM

0.5929 mL

2.9645 mL

5.9291 mL

10 mM

0.2965 mL

1.4823 mL

2.9645 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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (7.41 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (7.41 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 (281 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 Yi , et al. Discovery of a Small-Molecule Inhibitor Targeting the Androgen Receptor N-Terminal Domain for Castration-Resistant Prostate Cancer. 2023 May 4;22(5):570-582. [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	2.9645 mL	14.8227 mL	29.6454 mL	74.1136 mL
	5 mM	0.5929 mL	2.9645 mL	5.9291 mL	14.8227 mL
	10 mM	0.2965 mL	1.4823 mL	2.9645 mL	7.4114 mL
	15 mM	0.1976 mL	0.9882 mL	1.9764 mL	4.9409 mL
	20 mM	0.1482 mL	0.7411 mL	1.4823 mL	3.7057 mL
	25 mM	0.1186 mL	0.5929 mL	1.1858 mL	2.9645 mL
	30 mM	0.0988 mL	0.4941 mL	0.9882 mL	2.4705 mL
	40 mM	0.0741 mL	0.3706 mL	0.7411 mL	1.8528 mL
	50 mM	0.0593 mL	0.2965 mL	0.5929 mL	1.4823 mL
	60 mM	0.0494 mL	0.2470 mL	0.4941 mL	1.2352 mL
	80 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9264 mL
	100 mM	0.0296 mL	0.1482 mL	0.2965 mL	0.7411 mL

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SC428

MCE Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SC428 Related Classifications

HY-164373 Related Classifications