Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
AlkB homologue 5 (ALKBH5) IC50: 2.97 μM[1]
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ln Vitro |
DDO-2728 (0-40 μM, 48 h) increases m6A methylation levels in MOLM-13, HEK293 and MV4-11 cells over a concentration gradient [1]. DDO-2728 (0.01-100 μM, 72 h) can inhibit the proliferation of MOLM-13 and MV4-11 cells with IC50s of 0.45 and 1.2 μM respectively, and its toxicity to HEK293 and HUVEC is relatively weak [1]. DDO-2728 (20 μM, 48 h) significantly blocks the cell cycle of MOLM-13 and MV4-11 cells in the G1/M phase [1]. DDO-2728 (5, 10 μM, 48 h) induces apoptosis in MV4−11 and MOLM-13 cells in a concentration-dependent manner [1]. DDO-2728 (20 μM, 24 h) reduces the half-life of TACC3 mRNA in MOLM-13 and MV4−11 cells [1]. DDO-2728 (0-10 μM, 48 h) significantly reduces the abundance of TACC3 and c-Myc in MOLM-13 and MV4-11 cells at the mRNA and protein levels [1]. 1.19 Metabolic stability of rat and human plasma and liver microsomes [1]
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ln Vivo |
DDO-2728 (10-40 mg/kg, intraperitoneal injection, once daily, for 14 days) can effectively inhibit the growth of MV4−11 xenograft tumors in nude mice [1]. 1.19 Pharmacokinetic parameters of DDO-2728 in rats[1] Parameter Rat (iv, 2mg/kg) Rat (ip, 10mg/kg) T1/2 (min) 36.7 ± 3.2 148.3 ± 4.6 Cmax (ng/mL) 13388.3 ± 784.5 2337.5 ± 295.7 Tmax (min) 30 AUC0-∞ (min·μg/mL) 404.3 ± 58.6 349.1 ± 26.1 Vz_F_obs (mL/kg) 263.6 ± 17.5 6177.6 ± 650.2 Cl_F_obs (mL/min/kg) 5.0 ± 0.5 28.8 ± 2.2 MRT (min) 77.8 ± 15.5 168.2 ± 1.2 F (%) 17.3
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MOLM-13, MV4-11, HEK293, HUVEC Tested Concentrations: 0.01-100 μM Incubation Duration: 72 h Experimental Results: Inhibited the proliferation of MOLM-13 and MV4−11 cells with IC50s of 0.45 and 1.2 μM respectively, didn't show visual cytotoxicity in HEK293 and HUVECs under 1 μM. Apoptosis Analysis[1] Cell Types: MOLM-13 , MV4-11 Tested Concentrations: 0, 5, 10 μM Incubation Duration: 48 h Experimental Results: Induced cell apoptosis of MV4−11 and MOLM-13 cells concentration-dependently, apoptosis rate for MV4−11 increased from 7.17% to 55.4%, apoptosis rate for MOLM-13 increased from 6.49% to 31.5%. Cell Cycle Analysis[1] Cell Types: MOLM-13, MV4-11 Tested Concentrations: 20 μM Incubation Duration: 48 h Experimental Results: Arrested the cell cycle of MOLM-13 and MV4 −11 cells at the G1/M phase as no G2/M phase cells exist. |
Animal Protocol |
Animal/Disease Models: MV4−11 xenograft nude mice [1]
Doses: 10, 20, and 40 mg/kg Route of Administration: Intraperitoneal injection (i.p.) daily for 14 d Experimental Results: Inhibited tumor growth significantly even at a concentration of 10 mg/kg. No significant change in the weight of the mice and the main organs during the treatment, the organ weight of test group mice was the same as vehicle group, no obvious injury damage was observed in the HE staining images of organ tissues. |
References |
Molecular Formula |
C28H17F3N4O7
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Molecular Weight |
578.45
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CAS # |
3029515-97-4
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Appearance |
Typically exists as solids (or liquids in special cases) 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)
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Solubility (In Vitro) |
DMSO :~125 mg/mL (~216.09 mM; with sonication)
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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 | 1.7288 mL | 8.6438 mL | 17.2876 mL | |
5 mM | 0.3458 mL | 1.7288 mL | 3.4575 mL | |
10 mM | 0.1729 mL | 0.8644 mL | 1.7288 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.