| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Cereblon
CRBN (cereblon), an E3 ubiquitin ligase. |
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| ln Vitro |
As a cereblon-binding ligand-linker conjugate, Pomalidomide-C12-NH2 hydrochloride itself has no intrinsic biological activity; its function is to recruit the E3 ubiquitin ligase complex. When conjugated to a KRAS G12C-targeting ligand via the terminal primary amine (using amide bond formation), the resulting PROTAC KRAS G12C degrader-1 can simultaneously bind to both KRAS G12C and cereblon, leading to ubiquitination and subsequent proteasomal degradation of the KRAS G12C mutant protein. The long C12 alkyl linker provides the necessary distance and flexibility to bridge the KRAS G12C binding site and the cereblon recruitment site, enabling the formation of a productive ternary complex.
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| ln Vivo |
No specific in vivo activity has been reported for this conjugate alone; its in vivo degradation activity is observed only when conjugated to a KRAS G12C ligand to form the complete PROTAC KRAS G12C degrader-1 molecule. The in vivo efficacy of this PROTAC is being evaluated in KRAS G12C-driven cancer models.
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| Enzyme Assay |
N/A; this compound is not assessed in isolated enzyme/receptor binding assays. As a synthetic intermediate, its quality is confirmed by analytical methods such as HPLC and NMR, with a standard purity of ≥95-97%. Its binding affinity to cereblon is validated as part of the complete PROTAC KRAS G12C degrader-1 construct using biophysical methods such as surface plasmon resonance (SPR). The C12 alkyl linker can be characterized by mass spectrometry.
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| Cell Assay |
N/A; this conjugate is not tested alone in cell-based assays but is used as a building block for constructing PROTAC KRAS G12C degrader-1. In the synthesis of the complete PROTAC, the terminal primary amine is conjugated to a KRAS G12C-targeting ligand via amide bond formation using EDC/NHS or HATU. The resulting PROTAC is then tested in KRAS G12C-expressing cancer cells (e.g., NCI-H358 or MIA PaCa-2) for degradation activity by Western blotting to determine the DC50 (half-maximal degradation concentration). PROTAC KRAS G12C degrader-1 is a cereblon-based KRASG12C degrader.
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| Animal Protocol |
N/A; no animal studies are performed with the ligand-linker conjugate alone. For in vivo studies of PROTAC KRAS G12C degrader-1, the complete PROTAC molecule is formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline) and administered to animal models (e.g., mouse xenografts of KRAS G12C-driven cancers) via intraperitoneal (IP) or intravenous (IV) injection. Target degradation in tumors, tumor growth inhibition, and overall animal health are monitored. The long C12 alkyl linker is critical for the in vivo efficacy of the PROTAC.
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| ADME/Pharmacokinetics |
This compound has a molecular weight of 493.04, a molecular formula of C25H37ClN4O4, and a standard purity of ≥95-97%. It appears as a solid. For storage, it should be kept as a powder at -20degC for up to 3 years, protected from light. In a solvent, it can be stored at -80degC for 6 months or at -20degC for 1 month (protected from light). It is soluble in DMSO. The IUPAC name is 4-((12-aminododecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride. CAS: 2862774-02-3.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human or veterinary use. Standard chemical safety precautions should be followed during handling. The product has not been fully validated for medical applications. It is not an approved therapeutic drug and has not been cleared for clinical use. Pomalidomide is an immunomodulatory drug with known teratogenic effects; this derivative is for research purposes only.
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| References | |
| Additional Infomation |
The extremely long C12 alkyl linker (twelve-carbon chain) provides exceptional flexibility and distance between the cereblon ligand and the target protein ligand. This long linker was specifically optimized for the construction of PROTAC KRAS G12C degrader-1, which targets the oncogenic KRAS G12C mutant. KRAS is a small GTPase that is traditionally difficult to target with small molecules due to its lack of deep binding pockets, and PROTACs with long, flexible linkers have been shown to be effective at degrading this challenging target. This conjugate is a key building block for studying targeted degradation of KRAS G12C, which is an important driver mutation in non-small cell lung cancer, colorectal cancer, and pancreatic cancer.
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| Exact Mass |
492.25
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|---|---|
| CAS # |
2862774-02-3
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| PubChem CID |
164887439
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| Appearance |
Light yellow to green yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
34
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| Complexity |
698
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NCCCCCCCCCCCCN.Cl
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| InChi Key |
UURKWIVEDYHEIE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H36N4O4.ClH/c26-16-9-7-5-3-1-2-4-6-8-10-17-27-19-13-11-12-18-22(19)25(33)29(24(18)32)20-14-15-21(30)28-23(20)31;/h11-13,20,27H,1-10,14-17,26H2,(H,28,30,31);1H
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| Chemical Name |
4-(12-aminododecylamino)-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione;hydrochloride
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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.) |
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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