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CSRM617 hydrochloride

🥰Excellent
Catalog No. T10896LCas No. 1353749-74-2
Alias CSRM617 hydrochloride(787504-88-5 Free base)

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

CSRM617 hydrochloride

CSRM617 hydrochloride

🥰Excellent
Purity: 99.59%
Catalog No. T10896LAlias CSRM617 hydrochloride(787504-88-5 Free base)Cas No. 1353749-74-2
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$33In StockIn Stock
5 mg$52In StockIn Stock
10 mg$77In StockIn Stock
25 mg$156In StockIn Stock
50 mg$230In StockIn Stock
1 mL x 10 mM (in DMSO)$53In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.59%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].
In vitro
CSRM617 hydrochloride, within a concentration range of 0.01-100 μM applied over 48 hours, effectively inhibits the growth of various prostate cancer (PC) cell lines, including PC-3, 22RV1, LNCaP, and C4-2 cells. Furthermore, at concentrations of 10-20 μM over the same duration, it triggers concentration-dependent apoptosis in 22Rv1 cells, evidenced by cell death. Notably, a higher concentration of 20 μM administered for 72 hours leads to apoptosis in 22Rv1 cells, marked by the presence of cleaved Caspase-3 and PARP.
In vivo
CSRM617, administered orally at a dosage of 50 mg/kg daily for 20 days, significantly inhibits tumor growth in SCID mice with 22Rv1 xenografts. This regimen was observed to notably impede the development and proliferation of diffuse metastases in the tested animal model.
SynonymsCSRM617 hydrochloride(787504-88-5 Free base)
Chemical Properties
Molecular Weight291.69
FormulaC10H14ClN3O5
Cas No.1353749-74-2
SmilesCl.NC(CO)C(=O)N\N=C\c1ccc(O)c(O)c1O
Relative Density.1.68 g/cm3 at 21℃
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
DMSO: 45 mg/mL (154.27 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (6.86 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
DMSO
1mg5mg10mg50mg
1 mM3.4283 mL17.1415 mL34.2830 mL171.4149 mL
5 mM0.6857 mL3.4283 mL6.8566 mL34.2830 mL
10 mM0.3428 mL1.7141 mL3.4283 mL17.1415 mL
20 mM0.1714 mL0.8571 mL1.7141 mL8.5707 mL
50 mM0.0686 mL0.3428 mL0.6857 mL3.4283 mL
100 mM0.0343 mL0.1714 mL0.3428 mL1.7141 mL

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In Vivo Formulation Calculator (Clear solution)

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:
% DMSO
%
% Tween 80
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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

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