| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
At low doses, PS121912 functions as a VDR antagonist; however, at high concentrations, it reacts more strongly with the target, resulting in caspase 3/7 activation-mediated intercellular clearance [1]. By attaching to 1,25)-(OH)2D3, PS121912 lowers cyclins A and D's regulatory levels, putting HL-60 tip cells in the S phase or G2/M phase [1].
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| ln Vivo |
PS121912 has exhibited activation stability and can block the enzyme CYP3A4 at greater dosages in in vivo cancer tests [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Cancer cells composed of DU145 (prostate), Caco2 (colon), HL-60 (monocytes) and SKOV3 (ovary) Tested Concentrations: 0-100 μM Incubation Duration: 18 hrs (hours) Experimental Results: Induction of all Four types of cancer cells undergo apoptosis, among which HL-60 cells are the most sensitive. Cell proliferation assay[1] Cell Types: Four different cancer cell lines (DU145 prostate cancer, Caco2 colon cancer, SKOV3 ovarian cancer, and HL-60 monocytes) Tested Concentrations: 0.5, 2 μM Incubation Duration: 5 days Experimental Results: Zoom The growth inhibition of cancer cells caused by submicromolar concentrations of 1.25-(OH)2D itself does not have an anti-proliferative effect. Apoptosis analysis [1] Cell Types: HL-60 Cell Tested Concentrations: 500 nM Incubation Duration: 18 hrs (hours) Experimental Results: HSP60 and Survivin expression diminished, and pro-apoptotic BIM levels increased. RT-PCR[1] Cell Types: HL-60 Cell Tested Concentrations: 3 μM Incubation Duration: 18 h Experimental Results: Induced expression of caspase 3 and caspase 7 mRNA levels. |
| References |
| Molecular Formula |
C24H21F3N2O
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|---|---|
| Molecular Weight |
410.43
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| Exact Mass |
410.16
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| CAS # |
1529814-60-5
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| PubChem CID |
73334809
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C=CC(OC)=CC=1)(C1=C(NC2=CC=CC=C12)C)NC1C=CC(C(F)(F)F)=CC=1
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| InChi Key |
NNTQFFZNUZBJND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21F3N2O/c1-15-22(20-5-3-4-6-21(20)28-15)23(16-7-13-19(30-2)14-8-16)29-18-11-9-17(10-12-18)24(25,26)27/h3-14,23,28-29H,1-2H3
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| Chemical Name |
N-[(4-methoxyphenyl)-(2-methyl-1H-indol-3-yl)methyl]-4-(trifluoromethyl)aniline
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~243.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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