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Purity: ≥98%
Remetinostat (formerly known as SHP-141) is an inhibitor of histone deacetylase (HDAC) developed by Medivir as a topical application for use in early stage CTCL (Cutaneous T-cell lymphoma). HDAC inhibitors are not advised for use in early-stage patients because of their severe side effects, but they are approved for the treatment of CTCL in late-stage patients. Because of its special design, remetinostat can be applied topically and acts only on the skin. It is broken down as soon as it enters the bloodstream, so it doesn't have the negative effects of other HDAC inhibitors. Remetinostat showed promise in treating skin lesions, reducing itching, and improving patient compliance in patients with early-stage colorectal cancer (CTCL) in the phase II trial.
| Targets |
HDAC
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|---|---|
| ln Vitro |
In vitro activity: Kinase Assay: Cell Assay: |
| References | |
| Additional Infomation |
Remetinostat is under investigation in clinical trial NCT02213861 (Efficacy, Safety and Tolerability Study of SHAPE in IA, IB or IIA Cutaneous T-cell Lymphoma).
Remetinostat is a topical formulation containing the histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Upon cutaneous administration, SHP-141 selectively binds to and inhibits HDAC, resulting in an accumulation of highly acetylated histones in the skin (dermis and epidermis), the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes. These events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins. Topical administration of SHP-141 allows for high concentrations of this agent locally while minimizing systemic toxicity. |
| Molecular Formula |
C16H21NO6
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|---|---|---|
| Molecular Weight |
323.35
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| Exact Mass |
323.137
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| Elemental Analysis |
C, 59.43; H, 6.55; N, 4.33; O, 29.69
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| CAS # |
946150-57-8
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| Related CAS # |
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| PubChem CID |
24875489
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| Appearance |
White to off-white solid powder
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| LogP |
2.615
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
23
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(OC(CCCCCCC(NO)=O)=O)=CC=1)OC
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| InChi Key |
XDZAHHULFQIBFE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H21NO6/c1-22-16(20)12-8-10-13(11-9-12)23-15(19)7-5-3-2-4-6-14(18)17-21/h8-11,21H,2-7H2,1H3,(H,17,18)
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| Chemical Name |
methyl 4-[8-(hydroxyamino)-8-oxooctanoyl]oxybenzoate
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.73 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (7.73 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 25.0 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: ≥ 2.5 mg/mL (7.73 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 | 3.0926 mL | 15.4631 mL | 30.9262 mL | |
| 5 mM | 0.6185 mL | 3.0926 mL | 6.1852 mL | |
| 10 mM | 0.3093 mL | 1.5463 mL | 3.0926 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03875859 | Terminated | Drug: Remetinostat | Squamous Cell Carcinoma | Kavita Sarin | December 12, 2019 | Phase 2 |
| NCT03180528 | Completed | Drug: Remetinostat | Skin Basal Cell Carcinoma | Kavita Sarin | July 7, 2018 | Phase 2 |
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