Referencia número: HY-103053

PS121912

Revisión del cliente

Based on 1 Customer Validation

PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer.

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Pureza: 96.40%
No. CAS: 1529814-60-5
Fòrmula: C₂₄H₂₁F₃N₂O
Peso molecular:410.43

Almacenamiento:

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

PS121912 Chemical Structure

No. CAS: 1529814-60-5

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	0.59 μM Compound: PS121912	Inhibition of 1,25(OH)2D3-induced VDR (unknown origin)-mediated CYP24A1 transcription expressed in HEK293T cells after 16 hrs by luciferase reporter gene assay Inhibition of 1,25(OH)2D3-induced VDR (unknown origin)-mediated CYP24A1 transcription expressed in HEK293T cells after 16 hrs by luciferase reporter gene assay	[PMID: 24799995]
HEK-293T	IC₅₀	8.1 μM Compound: PS121912	Inhibition of 1,25(OH)2D3-induced VDR-LBD (unknown origin)-mediated GAL4-labeled SRC1 transcription expressed in HEK293T cells after 16 hrs by two-hydrid luciferase reporter gene assay Inhibition of 1,25(OH)2D3-induced VDR-LBD (unknown origin)-mediated GAL4-labeled SRC1 transcription expressed in HEK293T cells after 16 hrs by two-hydrid luciferase reporter gene assay	[PMID: 24799995]
HL-60	EC₅₀	20 μM Compound: PS121912	Cytotoxicity against human HL60 cells assessed as ATP level after 18 hrs by CellTiter-Glo assay Cytotoxicity against human HL60 cells assessed as ATP level after 18 hrs by CellTiter-Glo assay	[PMID: 24799995]
HL-60	EC₅₀	20 μM Compound: PS121912	Cytotoxicity against human HL60 cells assessed as cell viability after 18 hrs by CellTiter-Fluor assay Cytotoxicity against human HL60 cells assessed as cell viability after 18 hrs by CellTiter-Fluor assay	[PMID: 24799995]

In Vitro

PS121912 behaves like a VDR antagonist at low concentrations but interacts with more targets at higher concentrations leading to apoptosis mediated by caspase 3/7 activation^[1].
PS121912 (combined with 1,25-(OH)2D3)reduces the transcription levels of cyclin A and D thus arresting HL-60 cells in the S or G2/M phase^[1].

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

Cell Viability Assay^[1]

Cell Line:

Cancer cells consisting of DU145 (prostate), Caco2 (colon), HL-60 (monocytes), and SKOV3 (ovary)
Concentration:

0-100 μM
Incubation Time:

18 h
Result:

Induced apoptosis in all four cancer cells, with HL-60 cells being the most sensitive.

Cell Proliferation Assay^[1]

Cell Line:

Four different cancer cell lines (DU145 prostate cancer, Caco2 colon cancer, SKOV3 ovarian cancer and HL-60 monocytes)
Concentration:

0.5, 2 μM
Incubation Time:

5 days
Result:

Amplified the growth inhibition of cancer cells caused by 1.25-(OH)2Ds without being antiproliferative by itself at sub-micromolar concentrations.

Apoptosis Analysis^[1]

Cell Line:

HL-60 cells
Concentration:

500 nM
Incubation Time:

18 h
Result:

Reduced expression of HSP60 and Survivin and elevated the levels of pro-apoptotic BIM.

RT-PCR^[1]

Cell Line:

HL-60 cells
Concentration:

3 μM
Incubation Time:

18 h
Result:

Induced the expression of caspase 3 and caspase 7 mRNA levels.

In Vivo

PS121912 shows an acceptable metabolic stability and can inhibit the metabolic enzyme CYP3A4 at higher concentrations in vivo cancer studies^[1].

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

Chemical Information

No. CAS 1529814-60-5
Appearance Solid
Peso molecular 410.43
Fòrmula C₂₄H₂₁F₃N₂O
Color Off-white to light yellow
SMILES

FC(C1=CC=C(NC(C2=CC=C(OC)C=C2)C3=C(C)NC4=C3C=CC=C4)C=C1)(F)F
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (243.65 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

2.4365 mL

12.1823 mL

24.3647 mL

5 mM

0.4873 mL

2.4365 mL

4.8729 mL

10 mM

0.2436 mL

1.2182 mL

2.4365 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Sidhu PS, et al. Anticancer activity of VDR-coregulator inhibitor PS121912. Cancer Chemother Pharmacol. 2014;74(4):787-798. [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	2.4365 mL	12.1823 mL	24.3647 mL	60.9117 mL
	5 mM	0.4873 mL	2.4365 mL	4.8729 mL	12.1823 mL
	10 mM	0.2436 mL	1.2182 mL	2.4365 mL	6.0912 mL
	15 mM	0.1624 mL	0.8122 mL	1.6243 mL	4.0608 mL
	20 mM	0.1218 mL	0.6091 mL	1.2182 mL	3.0456 mL
	25 mM	0.0975 mL	0.4873 mL	0.9746 mL	2.4365 mL
	30 mM	0.0812 mL	0.4061 mL	0.8122 mL	2.0304 mL
	40 mM	0.0609 mL	0.3046 mL	0.6091 mL	1.5228 mL
	50 mM	0.0487 mL	0.2436 mL	0.4873 mL	1.2182 mL
	60 mM	0.0406 mL	0.2030 mL	0.4061 mL	1.0152 mL
	80 mM	0.0305 mL	0.1523 mL	0.3046 mL	0.7614 mL
	100 mM	0.0244 mL	0.1218 mL	0.2436 mL	0.6091 mL

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PS121912

Apoptosis Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors 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

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PS121912

Apoptosis Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors 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

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PS121912 Related Classifications

HY-103053 Related Classifications