| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
E3 ubiquitin ligase (CRBN). The CC‑885 moiety of the conjugate is a molecular glue degrader that binds to the E3 ligase cereblon (CRBN). It is designed to redirect the E3 ligase to a new target protein, leading to its ubiquitination and subsequent degradation by the proteasome.
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| ln Vitro |
In cell‑free assays, the CC‑885‑based degrader induces the ubiquitination of a target protein in the presence of the E3 ligase complex. The specificity and degradation activity are evaluated in cellular systems after conjugation to an antibody. In cell‑free assays, it can be used to assess the formation of a ternary complex between the degrader, the E3 ligase, and the target protein.
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| Enzyme Assay |
A general cell‑free protocol for assessing ternary complex formation: Recombinant CRBN‑DDB1 complex, His‑tagged target protein, and a donor/acceptor‑labeled antibody against the target are incubated with varying concentrations of the CC‑885‑based degrader. The formation of the ternary complex brings the donor and acceptor into close proximity, generating a TR‑FRET signal. The EC50 is calculated from the dose‑response curve.
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| Cell Assay |
A general cellular protocol for an AnDC: Target‑positive cancer cells are seeded in 12‑well plates. The AnDC (antibody conjugated to CC‑885‑CH2‑PEG1‑NH‑CH3) is added at concentrations of 0.01‑100 nM. After 24‑48 hours of incubation, the cells are harvested, and the levels of the target protein are assessed by Western blot. The DC50 (concentration for 50% degradation) and Dmax (maximal degradation) are calculated.
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| Animal Protocol |
General animal protocol for an AnDC: Nude mice bearing subcutaneous xenografts of target‑positive cancer cells are randomized into groups. The AnDC is administered intravenously at doses of 1, 3, and 10 mg/kg once weekly for three weeks. Tumor volume is measured twice weekly. At the end of the study, tumors are harvested for Western blot analysis to evaluate the degradation of the target protein and for IHC (Ki‑67, cleaved caspase‑3).
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| ADME/Pharmacokinetics |
General PK protocol for an AnDC: A PK study in cynomolgus monkeys would be performed after a single intravenous administration of the AnDC. Blood samples are collected over 21 days. The concentration of total antibody, conjugated antibody, and free degrader in serum are measured by ELISA and LC‑MS/MS. Key PK parameters such as clearance, half‑life, and AUC are determined.
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| Toxicity/Toxicokinetics |
General toxicity protocol for an AnDC: A 14‑day repeat‑dose intravenous toxicity study in rats would be performed at doses of 5, 15, and 50 mg/kg. Parameters include clinical signs, body weight, food consumption, hematology, serum chemistry, and histopathology of all major organs, with special attention to the bone marrow and gastrointestinal tract.
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| References | |
| Additional Infomation |
CC‑885‑CH2‑PEG1‑NH‑CH3 TFA is an innovative degrader used for the synthesis of antibody‑degrader conjugates (AnDCs). The TFA salt form improves its solubility. The CC‑885 moiety is a molecular glue degrader, and the PEG linker provides flexibility and solubility. It is a research chemical for the development of a novel class of targeted protein degradation therapeutics. The product is for research use only.
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| Molecular Formula |
C28H31CLF3N5O7
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|---|---|
| Molecular Weight |
642.02
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| Appearance |
Solid powder
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 1.5576 mL | 7.7879 mL | 15.5758 mL | |
| 5 mM | 0.3115 mL | 1.5576 mL | 3.1152 mL | |
| 10 mM | 0.1558 mL | 0.7788 mL | 1.5576 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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