2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. SC912

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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SC912 Chemical Structure

SC912 Chemical Structure

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Based on 1 publication(s) in Google Scholar

SC912 Related Antibodies

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Description

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[1].

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.

SC912 Related Antibodies

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.
Molecular Weight

493.27

Formula

C22H13Cl2F3N4O2
Appearance

Solid

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
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 (202.73 mM; Need ultrasonic; 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 2.0273 mL 10.1364 mL 20.2729 mL
5 mM 0.4055 mL 2.0273 mL 4.0546 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

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    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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 2.0273 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 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:

SC912SC 912SC-912Androgen ReceptorApoptosisAR-NTDcell cyclecastration-resistant prostate cancer(CRPC) cellLNCaP95 NOD-SCID miceInhibitorinhibitorinhibit

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