| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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IRX5183 (NRX-195183, VTP-195183, AGN-195183) is a potent, selective, and orally bioavailable retinoid acid receptor (RAR) alpha agonist with potential antineoplastic activity. Retinoid analogue NRX 195183 binds to and activates RAR alpha, modulating the transcription of genes responsible for cell differentiation and proliferation, which may result in cell differentiation, decreased cell proliferation, and the inhibition of tumorigenesis. Encoded by the RARA gene, RAR alpha is a nuclear receptor and a member of the steroid receptor superfamily.
| ln Vitro |
AGN-195183 (IRX-5183; Compound 4) suppresses the development of breast cancer cell lines and is inert in an in vivo model of local stimulation. AGN-195183 and ATRA limit the proliferation of human breast cancer cell lines T-47D and SK-BR-3. AGN-195183 does not produce local irritation caused by RARa-selective retinol Am-580. AGN-195183 is now in Phase I/IIA clinical trials in cancer patients.
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| References | |
| Additional Infomation |
RARalpha Agonist IRX5183 is an orally bioavailable retinoid acid receptor alpha (RARalpha) agonist and vitamin A derivative, with potential antineoplastic activity. Upon administration, RARalpha agonist IRX5183 binds to and activates RARalpha, which promotes RARalpha-mediated signaling. This results in the transcription of RARalpha-responsive genes, which are responsible for cellular differentiation and proliferation. This results in the induction of cellular differentiation and apoptosis, and leads to the inhibition of cellular proliferation and tumorigenesis. RARalpha is a nuclear receptor and a member of the steroid receptor superfamily; reduced RARalpha signaling is correlated with cancer development in a variety of cancer cell types.
Drug Indication Investigated for use/treatment in adverse effects (chemotherapy) and blood (blood forming organ disorders, unspecified). Mechanism of Action VTP-195183 is a retinoic acid receptor alpha (RARalpha) specific agonist. |
| Molecular Formula |
C22H22CLF2NO4
|
|---|---|
| Molecular Weight |
437.8642
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| Exact Mass |
437.12
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| CAS # |
367273-07-2
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| PubChem CID |
9867758
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
500.9±50.0 °C at 760 mmHg
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| Flash Point |
256.7±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.596
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| LogP |
9.02
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
30
|
| Complexity |
676
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PNAWUIKCVQSLFG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H22ClF2NO4/c1-21(2)5-6-22(3,4)16-12(21)9-11(18(27)17(16)23)19(28)26-10-7-13(24)15(20(29)30)14(25)8-10/h7-9,27H,5-6H2,1-4H3,(H,26,28)(H,29,30)
|
| Chemical Name |
4-(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)-2,6-difluorobenzoic acid
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| Synonyms |
NRX195183 NRX-195183 NRX
195183 IRX5183 IRX-5183 IRX 5183VTP-195183 VTP195183 VTP 195183 AGN-195183 AGN195183
AGN195183.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~11 mg/mL (~25.12 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.1 mg/mL (2.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.1 mg/mL (2.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.1 mg/mL (2.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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