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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 Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $854 | 8-10 weeks | |
50 mg | $1,110 | 8-10 weeks | |
100 mg | $1,780 | 8-10 weeks |
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) |
Molecular Weight | 437.86 |
Formula | C22H22ClF2NO4 |
Cas No. | 367273-07-2 |
Storage | Powder: -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
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