| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC FTO degrader 1 (Compound FP54) (0.08-2.5 μM, 48 h) degraded FTO in NB4 and MOLM-13 cells in a dose-dependent manner, with a maximum degradation rate >95%[1]. PROTAC FTO degrader 1 inhibited the proliferation of various acute myeloid leukemia cell lines, with IC50 values of 0.48-2.44 μM[1]. PROTAC FTO degrader 1 (2-5 μM, 48 h) significantly induced apoptosis in MOLM-13 and NB4 cells[1]. PROTAC FTO degrader 1 (5 μM) promoted the differentiation of MOLM-13 cells[1]. PROTAC FTO degrader 1 (2 μM, 48 h) increased the overall m6A modification level of mRNA in NB4 cells[1]. PROTAC FTO degrader 1 (2 μM, 48 h) reduced the multiribosome/80S monoribosome ratio in MOLM-13 cells and inhibited overall translation [1]. PROTAC FTO degrader 1 (2 μM) enriched the ribosomal biochemistry-related mRNAs MRPL36 and LYAR in YTHDF2 in MOLM-13 cells, reduced their mRNA stability, and promoted YTHDF2-mediated degradation [1].
|
|---|---|
| ln Vivo |
PROTAC FTO degrader 1 (Compound FP54) (25 mg/kg, intravenous injection, 3 times a week) delayed disease prediction in tumors in MA9.3Ras/MOLM13/AML-0148 mice and prolonged their survival [1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MOLM-13 and NB4 cells Tested Concentrations: 2 and 5 μM Incubation Duration: 48 h Experimental Results: Increased apoptotic cells. Induced cleavage of caspase-3 and PARP1. |
| Animal Protocol |
Animal/Disease Models: MA9.3Ras/ MOLM13/AML-0148 tumor mice models[1]
Doses: 25 mg/kg Route of Administration: Intraperitoneally injection, 3 times a week Experimental Results: Reduced AML cell engraftment in peripheral blood and bone marrow. Decreased leukemia burden and delayed disease onset. Prolonged survival. Showed no obvious toxicity to mouse body weight, blood routine, or major organs. |
| References |
| Molecular Formula |
C59H75CL2N9O10S
|
|---|---|
| Molecular Weight |
1173.25
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 0.8523 mL | 4.2617 mL | 8.5233 mL | |
| 5 mM | 0.1705 mL | 0.8523 mL | 1.7047 mL | |
| 10 mM | 0.0852 mL | 0.4262 mL | 0.8523 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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