| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC FAK degrader 3 (compound D4) (0-1000 nM, 24 h) can induce FAK degradation in PA-1, ID8, 4T1, H22, HEY, MDA-MB-231 and PLC/PRF5 cells. In PA-1 cells, 50 nM can induce 89% FAK degradation and 500 nM can induce 92% FAK degradation [1]. PROTAC FAK degrader 3 (1 μM) can inhibit the kinase activity of FAK (99%) (IC50 = 0.44 nM), STK33 (92%), CLK4 (87%) and Fes (86%) [1]. PROTAC FAK degrader 3 (0.01-100 μM, 72 h) has antiproliferative activity against PA-1, HEY and Huh-7 cells [1]. PROTAC FAK degrader 3 (0-3 μM, 1-7 days) reduced the colony formation, migration and invasion of PA-1 cells [1]. PROTAC FAK degrader 3 (3 μM, 24 hours) upregulated the expression of genes related to tumor immunogenicity, antigen presentation (HLA-B, HLA-F and B2M) and immunoproteasome-related genes (PSMB8 and PSMB9) in PA-1 cells [1]. PROTAC FAK degrader 3 (3 μM, 24 hours) promoted antigen presentation and MHC-I expression on the surface of ID8, PA-1, H22 and PLC/PRF5 cells [1]. PROTAC FAK degrader 3 (3 μM, 72 hours) promoted the activation and proliferation of antigen-specific CD8 T cells in ID8 cells co-cultured with activated mouse CD8 T cells [1].
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| ln Vivo |
PROTAC FAK degrader 3 (compound D4) (15 mg/kg, intraperitoneal injection, once daily for 8 days) enhances antitumor activity by promoting MHC-I expression and enhancing T cell activation in an H22 tumor mouse model [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: PA-1 cells Tested Concentrations: 0 nM, 0.14 nM, 0.41 nM, 1.23 nM, 3.7 nM, 11.1 nM, 33.3 nM, 100 nM Incubation Duration: 0 hours, 1 hour, 2 hours, 4 hours, 6 hours, 12 hours, 24 hours Experimental Results: Induced FAK degradation, almost completely degraded at 11.1 nM, and almost completely degraded at 24 hours. Western Blot analysis [1] Cell Types: ID8, 4T1, H22, HEY, MDA-MB-231 and PLC/PRF5 cells Tested Concentrations: 1 μM Incubation Duration: 24 hours Experimental Results: Induced FAK degradation. Western Blot Analysis [1] Cell Types: PA-1, H22 cells Tested Concentrations: 3, 10, 30 nM Incubation Duration: 24 hours Experimental Results: Induced FAK degradation, its degradation activity was comparable to GSK215 ( ), and more effective than BI-3663 ( ).
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| Animal Protocol |
Animal/Disease Models:H22 (1 × 106) tumor-bearing syngeneic mouse (6-week-old BALB/cJ) model [1]
Doses: 15 mg/kg Route of Administration: Intraperitoneal injection, once daily for 8 consecutive days Experimental Results: Inhibited tumor growth without affecting body weight, enhanced the expression of H2-Kd/H2-Dd on CD45- tumor cells (3.19 times higher than the vector), did not affect the expression of Pd-l1, and the expression level of CD107a was higher (2.82 times higher than the vector), indicating enhanced cytotoxicity. |
| References |
| Molecular Formula |
C48H50N8O9
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|---|---|
| Molecular Weight |
882.96
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C1CCC2=C1C(OC3=NC(NC4=CC=C(C=C4OC)C(NC5CCN(CC5)CCCCCCCOC6=C7C(C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=CC=C6)=O)=NC9=C3C=CN9)=CC=C2
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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 | 1.1326 mL | 5.6628 mL | 11.3255 mL | |
| 5 mM | 0.2265 mL | 1.1326 mL | 2.2651 mL | |
| 10 mM | 0.1133 mL | 0.5663 mL | 1.1326 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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