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AGN-195183

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

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 SizePriceAvailabilityQuantity
25 mg$8548-10 weeks
50 mg$1,1108-10 weeks
100 mg$1,7808-10 weeks
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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 growt
Targets&IC50
RARα:3 nM (Kd)
Chemical Properties
Molecular Weight437.86
FormulaC22H22ClF2NO4
Cas No.367273-07-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 62 mg/mL (141.60 mM)
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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