| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC FGFR3 Degrader-1 (48 h) effectively inhibited the proliferation of Huh-7, HepG2 and MHCC97-H liver cancer cells, with IC50 values of 0.56 μM, 1.44 μM and 1.87 μM, respectively [1]. PROTAC FGFR3 Degrader-1 (0.125-1 μM; 24 h) promoted dose-dependent degradation of FGFR3 protein in Huh-7 cells via the proteasome pathway, and this degradation process could be inhibited by combined treatment with B10 or pomalidomide [1]. PROTAC FGFR3 Degrader-1 (0.25-1 μM; 6-24 h) downregulated the expression of FGFR3 in Huh-7 cells in a time- and dose-dependent manner and inhibited the activity of the FGFR3/PI3K/AKT signaling pathway [1]. PROTAC FGFR3 degrader-1 (40 μM) stably binds to FGFR3 in Huh-7 cells, as demonstrated by its ability to protect FGFR3 from thermal denaturation in cell thermal denaturation assays [1]. PROTAC FGFR3 degrader-1 (10-40 μM) stably binds to FGFR3 in Huh-7 cell lysates, as demonstrated by its dose-dependent protective effect on FGFR3 in drug affinity-response target stability assays [1]. Molecular docking predictions showed that the binding energy of PROTAC FGFR3 degrader-1 to FGFR3 was -7.5 kcal/mol [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Huh-7 Tested Concentrations: 0.125–1 μM (degradation efficiency assessment); 1 μM (treatment alone for 24 hours); 10 μM MG132 (combined treatment); 1 μM B10 (combined treatment); 10 μM pomalidomide (combined treatment) Incubation Duration: 24 hours (1 μM treatment; combined treatment) Experimental Results: Promoted dose-dependent degradation of FGFR3 protein, with significant degradation observed at 0.5 μM and 1 μM. Treatment with MG132 in combination rescued its induced FGFR3 degradation, treatment with its precursor B10 in combination inhibited its induced FGFR3 degradation, and treatment with the CRBN E3 ligase ligand pomalidomide in combination inhibited its induced FGFR3 degradation. Western Blot Analysis [1] Cell Types: Huh-7 Tested Concentrations: 0.25-1 μM (dose-dependent assessment); 1 μM (time-dependent assessment) Incubation Duration: 6 h, 12 h, 24 h (1 μM treatment) Experimental Results: FGFR3 expression was downregulated, and PI3K/AKT pathway activity was inhibited in a time- and dose-dependent manner. Activation of FGFR3 significantly reversed its inhibitory effect on PI3K/AKT pathway activity. |
| References |
| Molecular Formula |
C46H53N9O5S
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|---|---|
| Molecular Weight |
844.04
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C1=CC2=C(N3C[C@@]4(CCCN5CCC[C@@]([C@@]54[H])([C@]3(CC2)[H])[H])[H])S1)NC6=C(C7=CN(CCCCNC8=CC=CC(C(N9C%10CCC(NC%10=O)=O)=O)=C8C9=O)N=N7)C=C(C(C)C)C=C6
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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 | 1.1848 mL | 5.9239 mL | 11.8478 mL | |
| 5 mM | 0.2370 mL | 1.1848 mL | 2.3696 mL | |
| 10 mM | 0.1185 mL | 0.5924 mL | 1.1848 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.
Products are for research use only; We do not sell to patients
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