| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
Dac590 (20 μM) completely inhibited the activity of recombinant FTO demethylase at a concentration of 20 μM [1]. Dac590 (0-1 μM; 0-48 h) increased the overall methylation level of m6A RNA in NB4 and MOLM-13 AML cells in a time- and dose-dependent manner [1]. Dac590 (0.2-5 μM) regulated the downstream oncogenic pathway of FTO in NB4 and MOLM-13 AML cells, upregulated the expression of ASB2 and RARA, and downregulated the expression of c-MYC and CEBPA [1]. Dac590 (0.5-1 μM; 48 h) induced myeloid differentiation in NB4 and MOLM-13 AML cells, manifested by increased CD11b expression [1]. Dac590 (1 μM; 48 h) can induce G1 phase cell cycle arrest in NB4 and MOLM-13 AML cells[1]. Dac590 (0.2-2 μM; 48 h) can induce dose-dependent apoptosis in NB4 and MOLM-13 AML cells[1]. Dac590 (0-1 μM; 48 h) can reduce the expression level of DNMT1 protein in NB4 and MOLM-13 AML cells[1]. Dac590 (72 h) can inhibit the proliferation of NB4, MOLM-13, NOMO-1, MV-4-11, HEL, U937, K562 and MONO-MAC-6 cells, with IC50 values of 327.7, 358.3, 1405, 506.1, 507.6, 845.1, 1191 and 596.5 nM, respectively[1].
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| ln Vivo |
Dac590 (25 and 40 mg/kg; gavage; daily; 20 days) significantly prolonged survival and inhibited tumor growth in the mouse MOLM-13 AML model [1]. No toxicity was observed in female BALB/c mice with Dac590 (40 mg/kg; gavage; daily; 28 days) [1].
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| Animal Protocol |
Animal/Disease Models:Female NSG mice (6 weeks old) were injected intravenously with MOLM-13 cells and pre-administered with 20 mg/kg busulfan [1] 24 hours prior.
Doses: 25, 40 mg/kg Route of Administration: Gavage; daily; 20 days Experimental Results: Survival was significantly prolonged compared to the vector control group. No adverse effects on body weight were observed. Survival benefit was enhanced when used in combination with decitabine (DAC). Animal/Disease Models:Female BALB/c mice (6-8 weeks old) [1] Doses: 40 mg/kg< Route of Administration: Gavage; daily; 28 days Experimental Results: No significant change in body weight compared to the solvent control group. No pathological changes were detected in the heart, liver, spleen, lungs, or kidneys by H&E staining. |
| References |
| Molecular Formula |
C19H16CLFN2O4
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|---|---|
| Molecular Weight |
390.79
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| CAS # |
3084407-00-8
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| Appearance |
Yellow to brown solid
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| SMILES |
OC(C1=CC(OC)=CC=C1NC2=C(C=C(C=C2Cl)C3=C(ON=C3C)C)F)=O
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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 : ~12.5 mg/mL (~31.99 mM; ultrasonic and warming and heat to 60°C)
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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 | 2.5589 mL | 12.7946 mL | 25.5892 mL | |
| 5 mM | 0.5118 mL | 2.5589 mL | 5.1178 mL | |
| 10 mM | 0.2559 mL | 1.2795 mL | 2.5589 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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