| ln Vitro |
A2073 (25-100 nM, 24-72 h) significantly inhibited the proliferation of HEL and K562 cells in a dose- and time-dependent manner, with IC50 values of 55.02 nM (HEL) and 77.07 nM (K562), respectively [1]. A2073 (25-100 nM, 24-72 h) reduced the number of HEL cells without significantly increasing apoptosis; it induced HEL cells to differentiate into erythroid cells, as evidenced by increased CD71 expression; and it caused cell cycle arrest while downregulating key cell cycle regulatory proteins [1]. A2073 (25-100 nM, 48 h) downregulated key proteins in the MAPK (RAS, RAF, MAPK, MEK), PI3K-AKT (PI3K, AKT), and NF-κB (p-NF-κB, p-IκBα) pathways [1]. A2073 forms stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1) [1].
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| ln Vivo |
A2073 (25-100 nM, 1-5 days) can effectively inhibit the proliferation of HEL cells in a zebrafish xenograft tumor model [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HEL cells Tested Concentrations: / Incubation Duration: 72 hours Experimental Results: Compared with cytarabine (Ara-C), this product can more effectively reduce the number of HEL cells, and the IC50 value is lower (55.02 nM vs. 73.36 nM) RT-PCR[1] Cell Types: HEL cells Tested Concentrations: 100 nM Incubation Duration: 48 hours Experimental Results: Increased the expression levels of erythroid differentiation markers GATA1, EKLF, SHIP1 and NFE2. Cell cycle analysis [1] Cell Types: HEL cells Tested Concentrations: 25, 50, 100 nM Incubation Duration: 24, 48, 72 hours Experimental Results: Caused cell cycle arrest in G0 and G2 phases, reducing the proportion of cells in S phase.
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| Animal Protocol |
Animal/Disease Models:CM-Dil-labeled HEL cells were transplanted into zebrafish embryos 48 hours after fertilization [1].
Doses: 25, 50, 100 nM Route of Administration: Days 1, 3, and 5 Experimental Results: No significant morphological abnormalities (morphology, survival rate, body length, and heart rate) were observed at any of the detection time points (days 1, 3, and 5) compared to the control group. No significant in vivo toxicity was induced in zebrafish embryos. HEL cell proliferation and migration were reduced. HEL cell proliferation was inhibited in a zebrafish xenograft model. |
| References |
| CAS # |
2834742-70-8
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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.) |
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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