Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
FGFR1 0.18 nM (IC50) FGFR2 1.2 nM (IC50) FGFR3 0.46 nM (IC50) FGFR4 1.4 nM (IC50) HDAC1 1.3 nM (IC50) HDAC2 1.6 nM (IC50) HDAC6 2.6 nM (IC50) HDAC8 13 nM (IC50)
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ln Vitro |
Compound 10e, HDAC-IN-50 (0.1, 1, 10, 100 nM; 12-84 h) promotes time- and dose-dependent apoptosis and cell cycle arrest in the G0/G1 phase[1]< /sup >. In a dose-dependent manner, HDAC-IN-50 (0, 1.25, 2.5, 5 µM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells; 36 h) decreases the expression of pFGFR1, pERK, and pSTAT3.
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ln Vivo |
Mice treated orally with HDAC-IN-50 (15, 30 mg/kg; once daily for 18 days) exhibit anti-tumor action [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HCT116, SNU-16, KATO III, A2780, K562, Jurkat cells Tested Concentrations: 0-30 µM Incubation Duration: 72 h Experimental Results: demonstrated antiproliferative activities with IC50s of 0.82, 0.0007, 0.0008, 0.04, 2.46, 15.14 µM for HCT116, SNU-16, KATO III, A2780, K562, Jurkat cells, respectively. Cell Cycle Analysis[1] Cell Types: SNU-16 cells Tested Concentrations: 0.1, 1, 10, 100 nM Incubation Duration: 12, 24, 36 h Experimental Results: Induced cell cycle arrest at G0/G1 phase in a time and dose-dependent manner. Apoptosis Analysis[1] Cell Types: SNU-16 cells Tested Concentrations: 0.1, 1, 10, 100 nM Incubation Duration: 36, 48, 60, 72, 84 h Experimental Results: Induced apoptosis with the apoptotic rate increased 30.8% and 49.6% at 10, 100 nM, respectively. Western Blot Analysis[1] Cell Types: HCT116, SNU-16 cells Tested Concentrations: 0, 1.25, 2.5, 5 µM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells Incubation Duration: 36 h Experimental Results: decreased the expression of pFGFR1, pERK, pSTAT3 in a dose-dependent manner. |
Animal Protocol |
Animal/Disease Models: BALB/c nude mice (HCT116 xenograft model)[1]
Doses: 15, 30 mg/kg Route of Administration: Po; daily for 18 days Experimental Results: Inhibited the tumor growth and downregulated the expression of pSTAT3, pFGFR1, increased the expression of Ac-H3. |
References |
[1]. Wan G, et al. Design and Synthesis of Fibroblast Growth Factor Receptor (FGFR) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Cancer. J Med Chem. 2022 Dec 22;65(24):16541-16569.
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Molecular Formula |
C31H41N7O4
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Molecular Weight |
575.70
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CAS # |
2653339-26-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
N1(CCCCCCC(NO)=O)C=C(C2C=NC3C(N=2)=CC(N(C2=CC(OC)=CC(OC)=C2)CCNC(C)C)=CC=3)C=N1
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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 | 1.7370 mL | 8.6851 mL | 17.3702 mL | |
5 mM | 0.3474 mL | 1.7370 mL | 3.4740 mL | |
10 mM | 0.1737 mL | 0.8685 mL | 1.7370 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.