| ln Vitro |
HDAC6-IN-74 (compound 14a) (0.05-50.0 μM; 72 hours) effectively inhibited the proliferation of HepG2 liver cancer cells, with an IC50 value of 0.7 μM. It showed low activity against Huh7 cells and no activity against LM3 cells, and exhibited high selectivity for tumor cells relative to non-tumor cell lines [1]. HDAC6-IN-74 (1-10 μM; 0-72 hours) induced apoptosis and S-phase cell cycle arrest in HepG2 cells and inhibited cell invasion and migration [1]. HDAC6-IN-74 (0-10.0 μM; 24 hours) downregulated the expression of HDAC6 and p-ERK1/2 in HepG2 cells and upregulated the expression of Ac-H3 and Ac-α-tubulin [1].
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| ln Vivo |
HDAC6-IN-74 (12.5-25.0 mg/kg; administered orally; every other day; 24 days) showed potent dose-dependent in vivo antitumor activity against xenograft tumors [1].
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice, HepG2 (female, 6 weeks old) [1] Treatment
Doses: 12.5 mg/kg; 25.0 mg/kg Route of Administration: Gavage; every other day; 24 days Experimental Results: The tumor inhibition rate reached 47.6% at the 12.5 mg/kg dose, the HDAC6 protein level in the tumor tissue was significantly reduced, the Ac-α-tubulin level in the tumor tissue was significantly increased, and tumor cell apoptosis was induced. The tumor inhibition rate reached 90.2%. Compared with the 12.5 mg/kg dose group, the HDAC6 protein level in the tumor tissue was significantly reduced, the Ac-α-tubulin level was increased to about 15.4 times that of the control group, and the level of tumor cell apoptosis induced in the 25 mg/kg dose group was the highest. No significant changes were observed in the body weight or histopathological abnormalities of major organs (heart, liver, spleen, lungs, and kidneys) in mice. |
| References |
| Appearance |
Typically exists as solids 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.) |
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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