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| Targets |
FAK (focal adhesion kinase). FC-11 is a PROTAC that recruits CRBN E3 ubiquitin ligase to FAK, leading to ubiquitination and subsequent proteasomal degradation of the FAK protein. This degradation-based mechanism eliminates both the enzymatic and scaffolding functions of FAK.
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| ln Vitro |
FC-11 is a highly potent FAK degrader with a DC90 (concentration required for 90% degradation) of 1 nM. DC50 values (half-maximal degradation concentration) vary by cell line: 40 pM in Ramos cells, 80 pM in PA1 cells, 310 pM in TM3 cells, 330 pM in MDA-MB-436 cells, and 370 pM in LNCaP cells. It effectively reduces FAK protein levels in multiple cancer cell lines.
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| ln Vivo |
FC-11 degrades FAK in multiple cancer cell lines with sub-nanomolar DC50 values. In xenograft mouse models, FC-11 has been used to investigate the non-enzymatic functions of FAK in tumor growth and metastasis. By eliminating FAK protein entirely rather than just inhibiting its kinase activity, FC-11 enables studies of FAK's scaffolding functions. The compound has shown efficacy in reducing tumor progression in preclinical models.
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| Enzyme Assay |
FC-11 is a PROTAC, so traditional cell-free enzyme activity assays are not directly applicable. For binding assays, the interaction of FC-11 with CRBN can be assessed using TR-FRET-based assays with recombinant CRBN-DDB1 complex. Alternatively, a ternary complex formation assay using purified FAK, CRBN-DDB1, and FC-11 can be performed, measuring complex formation by SPR or AlphaLISA. For FAK degradation, no enzyme activity readout is used; instead, residual FAK protein is quantified by Western blot.
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| Cell Assay |
Cancer cells (e.g., Ramos, PA1, TM3, MDA-MB-436, LNCaP) are seeded in 6-well or 96-well plates and treated with FC-11 at various concentrations (0.001-1000 nM) for 6-24 hours. After treatment, cells are lysed and FAK protein levels are quantified by Western blot using an anti-FAK antibody, normalized to a housekeeping protein (e.g., GAPDH). DC50 values are calculated from dose-response curves. Cell viability and proliferation are assessed by MTT or CellTiter-Glo assay. The effect of FAK degradation on downstream signaling (e.g., paxillin, Src, PI3K/AKT) can be analyzed by Western blot.
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| Animal Protocol |
For in vivo studies, FC-11 is administered to mice bearing xenograft tumors (e.g., PA1 ovarian cancer, MDA-MB-436 breast cancer). Dosing routes and regimens are not specified in available literature but likely involve intraperitoneal injection at doses of 5-20 mg/kg daily or every other day. Tumor volumes are measured with calipers. At study termination, tumors are excised and FAK protein levels are quantified by Western blot or immunohistochemistry to confirm target degradation. Pharmacodynamic markers such as paxillin phosphorylation are also assessed.
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| ADME/Pharmacokinetics |
No specific PK data are reported for FC-11. The molecular weight is 949.91 (C41H42F3N13O9S). The compound is a PROTAC, which typically has higher molecular weight than traditional small molecules, potentially affecting oral bioavailability. It is soluble in DMSO (50-100 mg/mL). For in vivo studies, FC-11 is typically formulated with co-solvents (e.g., PEG400, Tween-80). PK parameters (t1/2, Cmax, AUC, oral bioavailability, tissue distribution) have not been characterized. Storage: 4degC or -20degC, protect from light.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for FC-11. As a PROTAC degrader of FAK, potential toxicities include effects on normal cell adhesion, migration, and survival, as FAK plays critical roles in integrin signaling. In published in vivo studies at reported doses, no overt toxicity (significant weight loss, behavioral changes, mortality) has been reported. However, comprehensive toxicological assessments have not been performed. No FDA approval. No clinical trials.
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| References | |
| Additional Infomation |
Other information: FC-11 (CAS 2271035-37-9) is a research-grade PROTAC FAK degrader (DC90: 1 nM), not FDA-approved. It contains the CRBN ligand Pomalidomide and the FAK ligand PF562271. The compound is a powerful tool for investigating FAK-mediated signaling and non-enzymatic FAK functions in cancer research and therapeutic development. Synonyms: FC-11, FC 11. For research use only, not for human consumption.
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| Molecular Formula |
C41H42F3N13O9S
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|---|---|
| Molecular Weight |
949.914096355438
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| Exact Mass |
949.29
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| CAS # |
2271035-37-9
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| PubChem CID |
154723926
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
67
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| Complexity |
1850
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC=C(C=C3)NC(=O)C4=CN(N=N4)CCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)S(=O)(=O)C
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| InChi Key |
RZKZQCHSKWKOAJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C41H42F3N13O9S/c1-55(67(2,63)64)35-24(5-4-14-46-35)21-47-34-28(41(42,43)44)22-48-40(52-34)50-26-10-8-25(9-11-26)49-36(59)30-23-56(54-53-30)16-18-66-20-19-65-17-15-45-29-7-3-6-27-33(29)39(62)57(38(27)61)31-12-13-32(58)51-37(31)60/h3-11,14,22-23,31,45H,12-13,15-21H2,1-2H3,(H,49,59)(H,51,58,60)(H2,47,48,50,52)
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| Chemical Name |
1-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-N-[4-[[4-[[2-[methyl(methylsulfonyl)amino]pyridin-3-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]triazole-4-carboxamide
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 66.67 mg/mL (70.19 mM)
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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 | 1.0527 mL | 5.2637 mL | 10.5273 mL | |
| 5 mM | 0.2105 mL | 1.0527 mL | 2.1055 mL | |
| 10 mM | 0.1053 mL | 0.5264 mL | 1.0527 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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