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MI-136

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Catalog No. T6889Cas No. 1628316-74-4

MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.

MI-136

MI-136

😃Good
Purity: 99.12%
Catalog No. T6889Cas No. 1628316-74-4
MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$39In StockIn Stock
5 mg$89In StockIn Stock
10 mg$150In StockIn Stock
25 mg$293In StockIn Stock
50 mg$496In StockIn Stock
100 mg$768In StockIn Stock
200 mg$1,070-In Stock
1 mL x 10 mM (in DMSO)$98In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.12%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.
In vitro
MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage and blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer[1].
In vivo
Treatment of VCaP tumor-bearing mice with MI-136 (40 mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight[1].
Kinase Assay
HSP90 binding, ATPase, and selectivity profiling assays: The potency of HSP90 inhibitors for HSP90α, HSP90β, and Grp94 is determined by AlphaScreen competition binding assays, and activity against TRAP-1 is assessed by an ATPase assay.
Cell Research
To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM MI-136 for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and MI-136 for 48 hrs. Cells are then stimulated with 10 nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays. (Only for Reference)
Chemical Properties
Molecular Weight470.51
FormulaC23H21F3N6S
Cas No.1628316-74-4
SmilesFC(F)(F)Cc1cc2c(NC3CCN(Cc4ccc5[nH]c(cc5c4)C#N)CC3)ncnc2s1
Relative Density.1.45 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 87 mg/mL (184.91 mM), Sonication is recommended.
DMSO: 150 mg/mL (318.8 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.01 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.1254 mL10.6268 mL21.2535 mL106.2677 mL
5 mM0.4251 mL2.1254 mL4.2507 mL21.2535 mL
10 mM0.2125 mL1.0627 mL2.1254 mL10.6268 mL
20 mM0.1063 mL0.5313 mL1.0627 mL5.3134 mL
50 mM0.0425 mL0.2125 mL0.4251 mL2.1254 mL
100 mM0.0213 mL0.1063 mL0.2125 mL1.0627 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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