| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MYC-IN-4 (Compound 15) showed potent antiproliferative activity against PC-3 cells (MYC abnormal prostate cancer cells) with an IC50 value of 0.440 μM[1]. MYC-IN-4 (68 h) showed broad-spectrum antiproliferative activity against 14 other tumor cell lines, including MDA-MB-231, HCT-116, Myc-CaP, LN-CaP, NCI-H1581, A549, SK-N-BE, SK-OV-3, HepG-2, A-204, A-431, MG-63, LP-1 and MV4-11 cells, with IC50 values ranging from 0.331 μM to 2.60 μM[1]. MYC-IN-4 (10 μM, 1 h) significantly interfered with MYC/MAX protein-protein interaction (PPI) in PC-3 cells via Co-IP assay[1]. MYC-IN-4 (0.1–100 μM, 2 h) inhibited MYC/MAX PPI in cell-free AlphaLISA assay with an IC50 value of 3.06 μM[1]. MYC-IN-4 (10 μM, 1 h) reduced the thermostability of endogenous MYC in PC-3 cells[1]. MYC-IN-4 (1–10 μM, 24 h) induced concentration-dependent MYC degradation in PC-3 cells[1]. MYC-IN-4 inhibited MYC transcriptional activity in HEK293T cells transfected with E-box luciferase reporter plasmid with an IC50 value of 0.739 μM[1].
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|---|---|
| ln Vivo |
MYC-IN-4 (compound 15) (10-50 mg/kg, intraperitoneal injection, every other day for 16 days) showed potent antitumor activity in FVB carrying Myc-CaP-terminated tumor allografts [1].
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| Animal Protocol |
Animal/Disease Models: Myc-CaP cells (1 × 106 in 100 µL total volume) were subcutaneously implanted into the right flanks of 6-week-old male FVB mice to establish MYC-driven prostate tumor allograft models[1]
Doses: 10, 30, 50 mg/kg Route of Administration: i.p., QOD for 16 days Experimental Results: Achieved tumor growth inhibition (TGI) rates of 57% and 70% at doses of 30 mg/kg and 50 mg/kg. Showed no significant changes in body weight. Reduced the Ki67 expression. Combined with INCB086550 increased the infiltration of CD8⁺ T cells and CD45⁺ leukocytes in the tumor microenvironment. |
| References |
| Molecular Formula |
C19H10F6N2O2
|
|---|---|
| Molecular Weight |
412.29
|
| CAS # |
3109265-41-7
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| 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)
|
| 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 | 2.4255 mL | 12.1274 mL | 24.2548 mL | |
| 5 mM | 0.4851 mL | 2.4255 mL | 4.8510 mL | |
| 10 mM | 0.2425 mL | 1.2127 mL | 2.4255 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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