| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
HDAC6 8 nM (IC50) HDAC1 22 nM (IC50)
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|---|---|
| ln Vitro |
HDAC-IN-67 exhibits antiproliferative activity in tumor cells K562, MV4-11, HEL, SU-DHL-2 and WSU-DLCL-2 with IC50 values of 4.42 μM, 0.79 μM, 2.43 μM, 1.05 μM and 1.43 μM, respectively[1]. HDAC-IN-67 induces apoptosis in WSU-DLCL-2 cells (10 μM: 91.57%; 5 μM: 77.05%)[1].
|
| ln Vivo |
The clearance of HDAC-IN-67 (intravenous injection, 5 mg/kg) in ICR mice is 65.1 ml/(h·kg), and the elimination half-life is 0.361 hours[1]. The oral bioavailability of HDAC-IN-67 (oral administration, 10 mg/kg) is low (F=3.15%)[1]. HDAC-IN-67 (intraperitoneal injection, 50 mg/kg, for 21 days) has moderate antitumor efficacy in vivo, with a TGI of 31.5%[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: K562, MV4-11, HEL, SU-DHL-2 and WSU-DLCL-2 Tested Concentrations: 5 μM Incubation Duration: 72 h Experimental Results: Exhibited antiproliferative activity. Apoptosis Analysis[1] Cell Types: WSU-DLCL-2 Tested Concentrations: 5 μM and 10 μM Incubation Duration: 72 h Experimental Results: Induced WSU-DLCL-2 cells apoptosis in a dose-dependent manner (10 μM: 91.57%; 5 μM: 77.05%). |
| Animal Protocol |
Animal/Disease Models: Female ICR mice/antitumour potency[1]
Doses: i.p., 50 mg/kg once a day for 21 days Route of Administration: Intraperitoneal injection (i.p.) Experimental Results: Exhibited in vivo antitumorpotency with TGI of 31.5%. |
| References |
| CAS # |
2821923-75-3
|
|---|---|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
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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.
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