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[CAS NO. 367273-07-2] AGN-195183
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16684 |
| Brand: | MCE |
| CAS: | 367273-07-2 |
Overview
| MDL | MFCD18633237 |
|---|---|
| Molecular Weight | 437.86 |
| Molecular Formula | C22H22ClF2NO4 |
| SMILES | O=C(O)C1=C(F)C=C(NC(C2=C(O)C(Cl)=C3C(C)(C)CCC(C)(C)C3=C2)=O)C=C1F |
Summary
AGN-195183 (IRX-5183) is a potent and selective agonist of RARα ( K d =3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.
IC50 & Target
IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans)
In Vitro
AGN-195183 (IRX-5183; Compound 4) inhibits the growth of breast cancer cell lines, and is inactive in an in vivo model of topical irritation. AGN-195183 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3. AGN-195183 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. AGN-195183 is currently in Phase I/IIA clinical trials in cancer patients.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00234169 | Peter MacCallum Cancer Centre, Australia|The Leukemia and Lymphoma Society |
Multiple Myeloma|Lymphoma
|
October 2005 | Phase 1|Phase 2 |
| NCT00675870 | NuRx Pharmaceuticals, Inc. |
Acute Promyelocytic Leukemia
|
April 2008 | Phase 2 |
| NCT02749708 | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Io Therapeutics |
Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML)
|
January 30, 2017 | Phase 1 |
| NCT00670150 | University of Southern California|Sponsor Name Pending |
Acute Promyelocytic Leukemia
|
May 2010 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 11 mg/mL ( 25.12 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2838 mL | 11.4192 mL | 22.8384 mL |
| 5 mM | 0.4568 mL | 2.2838 mL | 4.5677 mL |
| 10 mM | 0.2284 mL | 1.1419 mL | 2.2838 mL |
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