| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Compound 4s, HDAC-IN-9, has anti-proliferative action against MCF-7, MGC-803, HeLa, A549, HepG2, and U937 cells, with IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, and 0.371 µM, respectively[1]. With IC50s of 10.89, 5.63, and 8.14 µM for 293 T, macrophages, and L02 cells, respectively, HDAC-IN-9 exhibits selectivity ratios of 6.1, 3.2, and 4.6 for these three types of cells[1]. With inhibitory concentrations of 6.8, 0.06, 0.12, and 8.5 µM for HDAC 1, HDAC 2, HDAC 6, and HDAC 10, respectively, HDAC-IN-9 exhibits inhibition actions against HDAC isoforms[1]. In A459 cells, HDAC-IN-9 (1, 2, 4 µM; 72 h) causes concentration-dependent cell cycle arrest at the G2/M phase[1]. In A549 cells, HDAC-IN-9 (1, 2, 4 µM; 72 h) promotes apoptosis through an intrinsic mitochondrial-mediated mechanism that is dependent on caspase[1]. HDAC-IN-9 (0, 0.5, 1, 2 µM; 48 h) inhibits angiogenesis and decreases endothelial cell metastasis in A549 cells, demonstrating anti-proliferative activity[1]. HDAC-IN-9 (0, 1, 2, 4 µM, 48 h) prevents A549 cells from invasively growing and migrating[1].
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| ln Vivo |
In zebrafish embryos, HDAC-IN-9 (0, 10, 20, 40 µM) inhibits the establishment of intersegmental blood vessels (ISVs)[1]. In zebrafish xenograft models, HDAC-IN-9 (0, 2.5, 5, 10 µM; 3 days) suppresses the growth and metastasis of A549 cells[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF -7, MGC-803, HeLa, A549, HepG2, U937 cells Tested Concentrations: Incubation Duration: 72 h Experimental Results: demonstrated anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC -803, HeLa, A549, HepG2, U937 cells, respectively). Cell Cycle Analysis[1] Cell Types: A459 cells Tested Concentrations: 0, 1, 2, 4 µM Incubation Duration: 72 h Experimental Results: Cells were arrested at the G2/ M phase with a dose-dependent manner. Apoptosis Analysis[1] Cell Types: A459 cells Tested Concentrations: 0, 1, 2, 4 µM Incubation Duration: 72 h Experimental Results: Induced apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells. Western Blot Analysis[1] Cell Types: A459 cells Tested Concentrations: 0, 1, 2, 4 µM Incubation Duration: 72 h Experimental Results: demonstrated down regulation of Cyclin B1 and Pcdc2 levels. |
| Animal Protocol |
Animal/Disease Models: embryos of Tg(flk:EGFP) transgenic zebrafish (transgenic zebrafish model Tg(flk1:EGFP))[1]
Doses: 0, 10, 20 , 40 µM Route of Administration: Experimental Results: Suppressed the formation of ISVs in zebrafish embryos. Animal/Disease Models: zebrafish xenograft models[1] Doses: 0, 2.5, 5, 10 µM Route of Administration: 3 days Experimental Results: Inhibited the proliferation and metastasis of A549 cells in zebrafish xenograft models. |
| References |
[1]. Sun M, et al. 2-Methoxydiol derivatives as new tubulin and HDAC dual-targeting inhibitors, displaying antitumor and antiangiogenic response. Bioorg Chem. 2022; 120:105625.
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| Molecular Formula |
C33H38N2O4
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|---|---|
| Molecular Weight |
526.67
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| Appearance |
Typically exists as solid at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8987 mL | 9.4936 mL | 18.9872 mL | |
| 5 mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8987 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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