| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
IHCH-3185 (compound 13t) inhibited recombinant human HDAC1 (IC50 = 102.9 nM, 15 min), had moderate inhibitory effects on HDAC2 and HDAC3, and had no inhibitory activity on HDAC4 or HDAC6 even at concentrations up to 10 μM [1]. IHCH-3185 inhibited the human A2AR receptor-mediated cAMP signaling pathway in HEK293-A2 AR cells with an IC50 of 88 nM [1]. IHCH-3185 showed broad-spectrum antiproliferative activity in various human and mouse tumor cell lines, with GI50 ranging from 0.06 μM (DoHH2) to 1.8 μM (MC38, SK-BR-3) [1]. IHCH-3185 (0.3–3.0 μM; 48 h) at concentrations of 0.3, 1.0, and 3.0 μM for 48 hours induced G0/G1 phase arrest in mouse colon cancer cell lines CT26 and HCT-116 in a concentration-dependent manner [1]. IHCH-3185 (1.5 nM; 72 h) reversed the inhibitory effect of NECA on IFN-γ secretion in activated mouse spleen cells after incubation for 72 hours [1]. IHCH-3185 (0.3–3.0 μM; 24 h) at concentrations of 0.3, 1.0, and 3.0 μM for 24 hours increased the levels of acetylated histone H3 and H4 in CT26 and MC38 mouse colon cancer cells in a concentration-dependent manner [1]. IHCH-3185 (1-10 μM; 24 h) upregulated the mRNA expression of H2-K1, Cxcl9 and Cxcl10 in MC38 mouse colon cancer cells in a concentration-dependent manner after treatment for 24 hours at concentrations of 1, 3 and 10 μM [1].
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| ln Vivo |
IHCH-3185 (compound 13t) (120 mg/kg; orally; once daily for 14 days) showed a tumor regression rate of 71.1% in the MC38 mouse model [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: CT26, MC38, GP-2d, SW620, HCT-116, T-47D, SK-BR-3, NCI-H1975, PC-9, SU-DHL-4, DoHH2 Tested Concentrations: 0.00005-10 μM Incubation Duration: 72 hours Experimental Results: Exhibited broad-spectrum anti-proliferative activity, with GI50 values of 0.38 μM (CT26), 1.8 μM (MC38), 0.6 μM (GP-2d), 0.6 μM (SW620), 0.2 μM (HCT-116), and 0.8 μM (T-47D), respectively. 1.8 μM (SK-BR-3), 0.5 μM (NCI-H1975), 0.4 μM (PC-9), 0.5 μM (SU-DHL-4), and 0.06 μM (DoHH2). Cell cycle analysis [1] Cell Types: CT26, HCT-116 mouse colon cancer cell lines Tested Concentrations: 0.3, 1.0, 3.0 μM Incubation Duration: 48 hours Experimental Results: Concentration-dependent G0/G1 phase arrest was induced in both CT26 and HCT-116 cells. At all tested concentrations, the proportion of cells in the G0/G1 phase increased significantly, while the proportion of cells in the S phase decreased accordingly. Western Blot Analysis [1] Cell Types: CT26 and MC38 mouse colon cancer cells Tested Concentrations: 0.3, 1.0, 3.0 μM Incubation Duration: 24 hours Experimental Results: Concentration-dependent increases in acetylated H3 and H4 levels were induced in both CT26 and MC38 cells, confirming the functional inhibition of HDAC.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 (male); BALB/c[1]
Doses: 60-120 mg/kg (MC38 model); 90-120 mg/kg (CT26 model); 20 mg/kg (PK); 100 mg/kg (PK); 5 mg/kg (PK, intravenous injection) Route of Administration: Oral; once daily; 14 days (antitumor efficacy); oral (PK, 20 mg/kg, 100 mg/kg); intravenous (PK, 5 mg/kg) Experimental Results: In the MC38 syngeneic mouse model, the target drug concentration (TGI) was 47.1% (P < 0.05) in the 60 mg/kg dose group, 62.2% (P < 0.01) in the 90 mg/kg dose group, and 71.1% (P < 0.01) in the 120 mg/kg dose group. (0.001). In the CT26 syngeneic mouse model, the TGI was 50.9% at the 90 mg/kg dose (P < 0.01) and 68.5% at the 120 mg/kg dose (P < 0.001). In male C57BL/6 mice, the oral bioavailability was 85% at the 20 mg/kg dose and 126% at the 100 mg/kg dose. In both CT26 and MC38 models, the number of regulatory T cells within the tumor was reduced, and the CD8+ T cell/Treg ratio was increased. Histone H3 acetylation was induced in CT26 and MC38 tumor tissues. None of the tested doses caused significant weight loss. |
| References |
| Molecular Formula |
C24H21N7O3
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|---|---|
| Molecular Weight |
455.47
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
NC1=NC(OCCC2=CC=C(C=C2)C(NC3=CC=CC=C3N)=O)=CC4=NC(C5=CC=CO5)=NN41
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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 | 2.1955 mL | 10.9777 mL | 21.9553 mL | |
| 5 mM | 0.4391 mL | 2.1955 mL | 4.3911 mL | |
| 10 mM | 0.2196 mL | 1.0978 mL | 2.1955 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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