| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CDK9/HDAC1/HDAC3-IN-1 (compound 13EA) (24 hours) showed potent antiproliferative activity in various cancer cell lines (e.g., IC50 values of 1.51 μM, 2.47 μM and 4.52 μM for HeLa, MDA-MB-231 and HepG2, respectively)[1]. CDK9/HDAC1/HDAC3-IN-1 (MDA-MB-231 cells: 0.625-5 μM, HeLa: 0.625-1.25 μM, 24 hours) inhibited the expression of p-Ser2 mRNA in MDA-MB-231 cells in a time- and dose-dependent manner[1]. CDK9/HDAC1/HDAC3-IN-1 (MDA-MB-231 cells: 0.625-5 μM, 24 h) significantly reduced the protein expression of p-Ser2 (a substrate of CDK9) in MDA-MB-231 cells and HeLa cells, while increasing the protein expression of Ac-H3 (a substrate of HDAC) [1]. CDK9/HDAC1/HDAC3-IN-1 (0.625-5 μM, 24 h) induced mitochondrial-related apoptosis in MDA-MB-231 cells and HeLa cells in a concentration-dependent manner, upregulated the expression of cleaved PARP, and arrested the cell cycle in the G2/M phase [1].
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|---|---|
| ln Vivo |
CDK9/HDAC1/HDAC3-IN-1 (30 mg/kg, intraperitoneal injection, once daily for 10 days) significantly inhibited tumor growth in the MDA-MB-231 mouse xenograft model [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: MDA-MB-231 cells, HeLa cells Tested Concentrations: MDA-MB-231 cells (0.625, 1.25, 2.5, 5 μM), HeLa cells (0.625, 1.25 μM) Incubation Duration: 24 hours Experimental Results: Dose-dependently inhibited p-Ser2 (a substrate of CDK9) levels and upregulated Ac-H3 (a substrate of HDAC) levels. Real-time quantitative PCR[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 0.625, 1.25, 2.5, 5 μM Incubation Duration: 3, 6, 12, 24 hours Experimental Experimental Results: CDK9 mRNA expression was downregulated in a time- and dose-dependent manner, reaching maximum inhibition at 24 hours. Immunofluorescence [1] Cell Types: MDA-MB-231 cells, HeLa cells Tested Concentrations: 3 μM Incubation Duration: 24 hours Experimental Results: p-Ser2 levels were decreased and Ac-H3 levels were upregulated in HeLa and MDA-MB-231 cells.
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| Animal Protocol |
Animal/Disease Models:MDA-MB-231 cells in logarithmic growth phase (3 × 10⁷ cells/mouse) were subcutaneously injected into 6-week-old female BALB/c nude mice [1].
Doses: 30 mg/kg Route of Administration: Intraperitoneal injection, once daily for 10 consecutive days until the tumor volume reached approximately 100 mm³. Experimental Results: The drug inhibited the growth of MDA-MB-231 xenograft tumors over time and significantly reduced tumor volume. Immunohistochemical staining showed a significant increase in cleaved caspase-3 and a significant decrease in PCNA levels in the tumor tissue. |
| References |
| Molecular Formula |
C24H22N8OS
|
|---|---|
| Molecular Weight |
470.55
|
| CAS # |
2197029-81-3
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CNC1=NC(C)=C(S1)C2=NC(NC3=CC=C4C(C=C(C(NC5=CC=CC=C5N)=O)N4)=C3)=NC=C2
|
| 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 | 2.1252 mL | 10.6259 mL | 21.2517 mL | |
| 5 mM | 0.4250 mL | 2.1252 mL | 4.2503 mL | |
| 10 mM | 0.2125 mL | 1.0626 mL | 2.1252 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.
Products are for research use only; We do not sell to patients
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