| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
DB818 targets the interaction between the transcription factor HOXA9 and DNA. HOXA9 is a transcription factor regulating hematopoiesis and leukemia cell proliferation. By binding in the DNA minor groove at HOXA9-cognate sites, DB818 blocks HOXA9/DNA interaction, inhibiting the growth of AML cells and inducing apoptosis.
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| ln Vitro |
In vitro, DB818 inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces apoptosis. Its activity is measured in cell viability and apoptosis assays using these cell lines. It inhibits HOXA9-mediated transcription.
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| ln Vivo |
In mice infected with worms, DB818 (12.5 mg/kg, 25 mg/kg; subcutaneously injected once daily for 4 days) totally eliminated parasitemia at the 25 mg/kg dose. Two thirds of the mice were cured at a dose of 12.5 mg/kg [1]. In mice, DB818 induces relapses approximately 20 days post-infection [1].
In vivo, DB818 is used as a research tool to study the role of HOXA9 in acute myeloid leukemia. Its ability to inhibit HOXA9 suggests it could be effective in animal models of AML. Specific in vivo data are not detailed. |
| Enzyme Assay |
The in vitro binding assay for DB818 involves measuring its ability to bind to DNA at HOXA9-cognate sites. This can be assessed using electrophoretic mobility shift assays (EMSA) or surface plasmon resonance. The compound's ability to block HOXA9/DNA interaction is a key measure of its activity.
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| Cell Assay |
In vitro cellular experiments for DB818 are conducted using AML cell lines such as OCI/AML3, MV4-11, and THP-1. Cells are treated with the compound, and cell proliferation and apoptosis are assessed. The effects on HOXA9-mediated transcription are measured by qRT-PCR.
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| Animal Protocol |
In vivo animal experiments for DB818 would involve using mouse xenograft models of AML. The compound would be administered, and tumor growth inhibition would be measured. The effects on HOXA9 target gene expression in tumors would be assessed.
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| References |
[1]. Sonoda Y, et al. Effects of HOXA9 Inhibitor DB818 on the Growth of Acute Myeloid Leukaemia Cells. Anticancer Res. 2021 Apr;41(4):1841-1847.
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| Exact Mass |
256.0648
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|---|---|
| Appearance |
White to yellow solid powder
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| Synonyms |
DB818 DB-818 DB 818
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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.) |
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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