| Size | Price | Stock | Qty |
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Tefinostat (CHR-2845) is a novel and potent histone deacetylase inhibitor (HDACi) with anticancer activity. As a monocyte/macrophage-targeted pan HDAC inhibitor, it has to be cleaved into active acid form CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1).
| ln Vitro |
Tefinostat (CHR-2845) (1-4 nM) has an EC50 value of 2.3 μM, 57 nM, 110 nM, and 560 nM, respectively, and is active against the AML cell lines HL60 (M2 FAB type), MV411 (M4, FLT3-ITD), OCIAML3 (M4 NPM1mut), and THP1 (M5) [1]. Tefinostat exhibits substantial growth inhibition and dose-dependent induction of apoptosis at 0, 0.5, 1, and 5μM for 24 and 48 hours [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: AML cell line Tested Concentrations: 1-4 nM Incubation Duration: Experimental Results: Significant growth inhibition. Apoptosis analysis [1] Cell Types: Myeloid mononuclear cell line and HL60 Cell Tested Concentrations: 0, 0.5, 1 and 5μM Incubation Duration: 24, 48 hrs (hours) Experimental Results: In myeloid mononuclear cell line THP1, MV411 (FLT3-ITD) and OCIAML3 acted within 24 hrs (hours) and reached higher concentrations only in non-monocyte HL60 cells. |
| References | |
| Additional Infomation |
Tefinostat is under investigation in clinical trial NCT02759601 (Dose Escalation Trial of Tefinostat for Cancer Associated Inflamation in Hepatocellular Carcinoma (HCC)).
Tefinostat is a hydroxamic acid-derived histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Tefinostat inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in chromatin remodeling, inhibition of tumor oncogene transcription, inhibition of tumor cell division, and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins; this agent may specifically target HDACs in cells of the monocyte-macrophage lineage. |
| Molecular Formula |
C28H37N3O5
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|---|---|
| Molecular Weight |
495.62
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| Exact Mass |
495.273
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| CAS # |
914382-60-8
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| PubChem CID |
15940949
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| Appearance |
White to off-white solid powder
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| LogP |
6.092
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
36
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| Complexity |
668
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CCC(C1)OC(=O)[C@H](C2=CC=CC=C2)NCC3=CC=C(C=C3)NC(=O)CCCCCCC(=O)NO
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| InChi Key |
GLNWREBYRLDPQP-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C28H37N3O5/c32-25(14-6-1-2-7-15-26(33)31-35)30-23-18-16-21(17-19-23)20-29-27(22-10-4-3-5-11-22)28(34)36-24-12-8-9-13-24/h3-5,10-11,16-19,24,27,29,35H,1-2,6-9,12-15,20H2,(H,30,32)(H,31,33)/t27-/m0/s1
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| Chemical Name |
cyclopentyl (2S)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate
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| Synonyms |
CHR2845 CHR 2845 CHR-2845
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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 : ~100 mg/mL (~201.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 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 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 (5.04 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: ≥ 0.83 mg/mL (1.67 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 | 2.0177 mL | 10.0884 mL | 20.1767 mL | |
| 5 mM | 0.4035 mL | 2.0177 mL | 4.0353 mL | |
| 10 mM | 0.2018 mL | 1.0088 mL | 2.0177 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.
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