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| ln Vitro |
RUNX1/ETO is made up of four neural homology regions (NHR1-4) that are produced by the ETO gene and DNA-binding Runt domain 5, which is the result of the RUNX1 gene. RUNX1/ETO tetramerization is brought about by the NHR2 domain. The vitality of RUNX1/ETO-dependent human leukemia SKNO-1 cells is preferentially reduced by RUNX1/ETO tetramer-IN-1 (compound 7.44) at 1 μM and 10 μM; 3, 5, 7 d [1]. U937 cells are not affected in the same way. Compound 7.44, which is the RUNX1/ETO tetramer-IN-1, suppresses the proliferation of RUNX1/ETO-expressing cells (SKNO-1, Kasumi-1, and K562) and induces myeloid differentiation at 25 μM and 50 μM, respectively, in five days. 2.]. RUNX1/ETO tetramer-IN-1 (100 μM; 7 d) causes RUNX1/ETOtr-expressing CD34+ progenitor cells to differentiate and enter a growth arrest [2]. Compound 7.44, also known as RUNX1/ETO tetramerization-IN-1, exhibits favorable physicochemical and ADME characteristics, as well as high water solubility, significant stability in buffer and plasma, minimal hepatic clearance in vitro, and water solubility of 60 μg/mL[3]. CYP2B6, 2C9, 2C19, and 3A4 may be inhibited by RUNX1/ETO tetramer-IN-1 (1 μM and 10 μM) [3]. RUNX1/ETO tetramer-IN-1 (compound 8) (50 μM; 16 hours) impacts the JNK pathway in cells and inhibits c-Jun N-terminal kinase (JNK) [4].
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| ln Vivo |
RUNX1/ETO tetramerized-IN-1 (compound 7.44) (200-250 μg/kg; i.p.; 5 times per week; 130 days) delays tumor growth of mouse RUNX1/ETO cells [2].
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| Cell Assay |
Cell viability assay [1]
Cell Types: RUNX1/ETO-dependent human leukemia SKNO-1 and U937 cells Tested Concentrations: 1 μM and 10 μM Incubation Duration: 3, 5, 7 days Experimental Results: Specific inhibition of SKNO-1 cell growth. Cell viability assay[3] Cell Types: RUNX1/ETO Pharmacokinetic Properties of Tetramer-IN-1 Tested Concentrations: Incubation Duration: Experimental Results: Kinetic Solubility (99% PBS, 1% DMSO) 177 µM Plasma Protein Binding ( Mouse plasma, 60 minutes) 98.4% Plasma stability (mouse plasma, 0–240 minutes) No degradation Hepatocyte stability (mouse hepatocytes) 2.5 µL/min/million cells Chemical stability in PBS (0 –4 hrs (hours)) No degradation |
| Animal Protocol |
Animal/Disease Models: NSG immunodeficient mice (NOD.Cg-Prkdcscid Il2rgtm1WjI/SzJ) injected with Kasumi-1 cells [2]
Doses: 200-250 μg/Kg Route of Administration: intraperitoneal (ip) injection; 5 times a week for 130 days. Experimental Results: Reduces the spread of leukemia cells, with 75% of mice still alive on day 130 after treatment. |
| References |
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| Molecular Formula |
C18H14O7
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|---|---|
| Molecular Weight |
342.299565792084
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| Exact Mass |
342.074
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| CAS # |
88755-39-9
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| PubChem CID |
294348
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| Appearance |
White to off-white solid powder
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| Density |
1.472g/cm3
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| Boiling Point |
598.6ºC at 760 mmHg
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| Flash Point |
223.2ºC
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| Index of Refraction |
1.641
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| LogP |
2.585
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
522
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PPEBBOHQEAQKSW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14O7/c19-13(11-2-4-15-17(6-11)25-9-23-15)7-12(18(20)21)10-1-3-14-16(5-10)24-8-22-14/h1-6,12H,7-9H2,(H,20,21)
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| Chemical Name |
2,4-bis(1,3-benzodioxol-5-yl)-4-oxobutanoic acid
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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 | 2.9214 mL | 14.6071 mL | 29.2141 mL | |
| 5 mM | 0.5843 mL | 2.9214 mL | 5.8428 mL | |
| 10 mM | 0.2921 mL | 1.4607 mL | 2.9214 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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