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AGN-195183

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Catalog No. T14144Cas No. 367273-07-2

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients. Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, however it does not cause the topical irritation induced by the RARa-selective retinoid, Am-580.

AGN-195183

AGN-195183

😃Good
Catalog No. T14144Cas No. 367273-07-2
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients. Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, however it does not cause the topical irritation induced by the RARa-selective retinoid, Am-580.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$8548-10 weeks8-10 weeks
50 mg$1,1108-10 weeks8-10 weeks
100 mg$1,7808-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients. Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, however it does not cause the topical irritation induced by the RARa-selective retinoid, Am-580.
Targets&IC50
RARα:3 nM (Kd)
Chemical Properties
Molecular Weight437.86
FormulaC22H22ClF2NO4
Cas No.367273-07-2
Relative Density.1.354 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
DMSO: 62 mg/mL (141.6 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.67 mg/mL (3.81 mM), Sonication is recommeded.
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 mM2.2838 mL11.4192 mL22.8384 mL114.1918 mL
5 mM0.4568 mL2.2838 mL4.5677 mL22.8384 mL
10 mM0.2284 mL1.1419 mL2.2838 mL11.4192 mL
20 mM0.1142 mL0.5710 mL1.1419 mL5.7096 mL
50 mM0.0457 mL0.2284 mL0.4568 mL2.2838 mL
100 mM0.0228 mL0.1142 mL0.2284 mL1.1419 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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
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Keywords

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