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| ln Vitro |
FKBP12 PROTAC FM4 (0.001-100 nM; 24 hours) efficiently and selectively degrades BRD4-FKBP12 transiently transfected in HEK293T cells via the VHL- or CRBN-dependent proteasome pathway, with DC50 values of 0.09-0.22 nM and maximum degradation rates of 90% and 81% respectively over 24 hours, and no cytotoxicity was observed at concentrations up to 100 nM [1]. FKBP12 PROTAC FM4 (0.001-100 nM; 24 hours) degrades MST2-FKBP12 transiently transfected in HEK293T cells via the CRBN-dependent proteasome pathway, with a maximum degradation rate of 80% over 24 hours, while VHL-MTH1 showed very low activity against this target [1]. FKBP12 PROTAC FM4 (0.001-100 nM; 24 hours) degrades KRAS-FKBP12 transiently transfected in HEK293T cells via the VHL or CRBN-dependent proteasome pathway. After 24 hours, the maximum degradation rate of VHL-MTH1 was 59%, and the degradation depended on the proximity of the dimerizing tags [1]. FKBP12 PROTAC FM4 (0.001-100 nM; 24 hours) induces dose-dependent degradation of BRD4 and MST2 in transiently transfected HEK293T cells via various viral E3 ligases. After 24 hours, the maximum degradation rate was 50% to 89%, and the degradation depended on the proteasome [1]. FKBP12 PROTAC FM4 (0.001-100 nM; 24 hours) degraded multiple pan-essential proteins in transiently transfected HEK293T cells via the MTH1-E6 pathway. Among them, SARS1 and eIF2S1 showed a maximum degradation rate of over 60% at 24 hours, and this degradation depended on the interaction between E6 and E6AP [1]. FKBP12 PROTAC FM4 (0.0001-100 nM; 6, 48 hours) selectively induced proteasome-dependent SARS1 degradation, inhibited protein synthesis, triggered apoptosis, and reduced the cell viability of C33ASARS1-FH:E6 cervical cancer cells with an EC50 value of 0.2 nM, while having no effect on parental cells, indicating that it has disease-specific targeted protein degradation effects [1].
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| References |
| Molecular Formula |
C73H89N7O17
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|---|---|
| Molecular Weight |
1336.52
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| CAS # |
3115268-06-6
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| Appearance |
Light yellow to green yellow solid
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| SMILES |
CC[C@@H](C1=CC(OC)=C(C(OC)=C1)OC)C(N2CCCC[C@H]2C(O[C@@H](C3=CC=CC(OCCNC(COCCOCCOCCOCCOCCNC(C4=CC=C(C=N4)C5=CC=C6N=CC(C(NC)=O)=C(C6=C5)NC7=CC=CC=C7)=O)=O)=C3)CCC8=CC(OC)=C(C=C8)OC)=O)=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 Note: 请将本产品存放在密封且受保护的环境中（例如氮气下），避免暴露在潮湿和光照下。 |
| 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 : ~50 mg/mL (~37.41 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 | 0.7482 mL | 3.7411 mL | 7.4821 mL | |
| 5 mM | 0.1496 mL | 0.7482 mL | 1.4964 mL | |
| 10 mM | 0.0748 mL | 0.3741 mL | 0.7482 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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