| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
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| Targets |
BRD4 BD1 3869 nM (IC50); BRD4 BD2 5.8 nM (IC50); BRD3 BD2 70.98 nM (Ki)
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|---|---|
| ln Vitro |
XY221 inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2, BRDT BD2 and BRD4 BD1 with IC50 values of 5.8, 70.98, 53.47, 183, 3869 nM, respectively[1]. XY221 inhibits the proliferation of MV4−11, LNCaP, and HL-7702 cells with IC50 values of 0.51, 0.68, and 47.7 μM, respectively[1]. XY221 (500-2000 nM, 72 h) can significantly inhibit the proliferation of MV4-11 cells and induce apoptosis of MV4-11 cells[1]. The half-life of XY221 (1-10 μM, 2 h) is more than 120 min in RLM (rat liver mitochondria) and more than 120 min in HLM (human liver mitochondria) [1]. XY221 (500-2000 nM, 72h) inhibits the phosphorylation of target genes p21, ODC1, BRD4, AKT and AMPK in MV4−11 cells [1]. XY221 (2 μM, 72h) inhibits the expression of the oncogene MYC and its target gene p21 and the cell cycle-related gene BCL-2 in MV4−11 cells at the mRNA level[1].
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| ln Vivo |
Pharmacokinetic parameters of XY221 in rats after intravenous (iv) and oral (po) administration route Cmax (μg/L) Tmax (h) AUC (0-t) (μg/L・h) AUC (0-∞) (μg/L・h) T1/2 (h) CI (L/h/kg) F (%) XY221 iv (5 mg/kg) 9790 0.03 4291 4294 1.35 1.21 XY221 po (25 mg/kg) 567 3.67 2811 2816 2.13 13.1
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MV4−11 cells Tested Tested Concentrations: 500, 2000 nM Incubation Duration: 24-72 h Experimental Results: Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK. Real Time qPCR[1] Cell Types: MV4−11 cells Tested Tested Concentrations: 2 μM Incubation Duration: 72 h Experimental Results: Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK. Suppressed oncogene MYC and its target gene p21 and cell-cycle-related gene BCL-2 at mRNA level. |
| References |
| Molecular Formula |
C32H34FN3O5
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|---|---|
| Molecular Weight |
559.63
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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)
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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 | 1.7869 mL | 8.9345 mL | 17.8689 mL | |
| 5 mM | 0.3574 mL | 1.7869 mL | 3.5738 mL | |
| 10 mM | 0.1787 mL | 0.8934 mL | 1.7869 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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