2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. SC428

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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SC428 Chemical Structure

SC428 Chemical Structure

CAS No. : 1898232-70-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

SC428 Related Antibodies

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Description

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[1].

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.

SC428 Related Antibodies

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.
Molecular Weight

337.32

Formula

C15H10F3N3OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

N#CC1=CC=C(NC(N/C=C/C2=CC=CS2)=O)C=C1C(F)(F)F
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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9645 mL 14.8227 mL 29.6454 mL
5 mM 0.5929 mL 2.9645 mL 5.9291 mL
View the 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.

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In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SC4281898232-70-6SC 428SC-428Androgen ReceptorApoptosisAndrogen receptor inhibitorAR ligand-binding domain (LBD) Prostate cancerResistance mechanismsInhibitorinhibitorinhibit

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