| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Not applicable. SC209 intermediate-1 is a chemical linker precursor for ADC synthesis, not a drug. It has no specific biological target. Its purpose is to connect a cytotoxic payload to an antibody for targeted cancer therapy. The intermediate contains reactive functional groups that enable controlled conjugation, ultimately linking the antibody to the payload via a stable bond.
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|---|---|
| ln Vitro |
As an ADC linker precursor, SC209 intermediate-1 has no direct biological activity. Its value lies in enabling the synthesis of stable and functional ADCs. The resulting ADCs exhibit potent cytotoxicity against target antigen-positive cancer cells, while the linker ensures stability in circulation and controlled release of the payload at the tumor site. The purity of the linker is typically ≥98%.
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| ln Vivo |
No specific in vivo data is reported for SC209 intermediate-1. As a linker intermediate, it is not studied directly in vivo. However, ADCs synthesized using this linker have demonstrated efficacy in tumor xenograft models, with tumor growth inhibition and minimal off-target toxicity. The linker's stability in serum is a key parameter studied.
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| Enzyme Assay |
Not applicable. SC209 intermediate-1 is a chemical reagent used in organic synthesis for bioconjugation. A typical conjugation protocol involves first activating the ADC linker or coupling it to a cytotoxic payload using standard amide bond formation chemistry (e.g., EDC/HOBt). The resulting drug-linker conjugate is purified by HPLC and then conjugated to a monoclonal antibody via a reactive functional group (e.g., maleimide-thiol chemistry). The final ADC is characterized by SEC-HPLC and LC-MS.
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| Cell Assay |
Not applicable. SC209 intermediate-1 itself is not used in cell-based assays. The final ADC produced using this linker is tested in vitro. Target-positive and target-negative cancer cells are seeded in 96-well plates (5,000 cells/well) and treated with serial dilutions of the ADC (1 pM to 100 nM) for 72-96 hours. Cell viability is measured using the CellTiter-Glo assay. A selectivity index is calculated based on IC50 values on target-positive vs. target-negative cells.
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| Animal Protocol |
No specific in vivo animal study protocols are documented for SC209 intermediate-1 itself. For an ADC synthesized with this linker, a typical protocol involves establishing subcutaneous xenografts of target-positive cancer cells in 6-8 week old female NSG mice. When tumors reach 100-150 mm3, the ADC is administered intravenously at a single dose of 1-10 mg/kg. Tumor growth inhibition (TGI) and survival are monitored for up to 60 days post-dose. Blood is collected for PK analysis and to assess linker stability in circulation.
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| ADME/Pharmacokinetics |
Not applicable for the intermediate. As a small molecule with a molecular weight of 406.47 g/mol, the intermediate itself is a solid that is soluble in DMSO. In ADC development, the final conjugated antibody retains the favorable PK properties of the monoclonal antibody, with a typical half-life of 7-14 days in mice. The linker ensures that the conjugate remains stable in circulation.
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| Toxicity/Toxicokinetics |
No toxicity data is reported for SC209 intermediate-1. As a chemical intermediate, standard safety precautions (gloves, goggles, fume hood) should be used. The compound is for research and manufacturing use only, not for human or veterinary therapeutic application.
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| References | |
| Additional Infomation |
SC209 intermediate-1 (Compound A7a) has the molecular formula C21H30N2O6 and a molecular weight of 406.47. The IUPAC name is (2S)-3-methyl-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]-3-[3-(prop-2-enoxycarbonylamino)phenyl]butanoic acid. It is an off-white to yellow solid. The compound serves as a building block for ADC linker synthesis, enabling the production of stable antibody-drug conjugates for targeted cancer therapy.
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| Molecular Formula |
C21H30N2O6
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|---|---|
| Molecular Weight |
406.472706317902
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| Exact Mass |
406.21
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| CAS # |
1977557-93-9
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| PubChem CID |
122467586
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| Appearance |
Off-white to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
29
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| Complexity |
611
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)(C)OC(=O)N(C)[C@H](C(=O)O)C(C)(C)C1=CC(=CC=C1)NC(=O)OCC=C
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| InChi Key |
WZSKLNHEJZJMLY-MRXNPFEDSA-N
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| InChi Code |
InChI=1S/C21H30N2O6/c1-8-12-28-18(26)22-15-11-9-10-14(13-15)21(5,6)16(17(24)25)23(7)19(27)29-20(2,3)4/h8-11,13,16H,1,12H2,2-7H3,(H,22,26)(H,24,25)/t16-/m1/s1
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| Chemical Name |
(2S)-3-methyl-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]-3-[3-(prop-2-enoxycarbonylamino)phenyl]butanoic acid
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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. |
| 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 | 2.4602 mL | 12.3010 mL | 24.6021 mL | |
| 5 mM | 0.4920 mL | 2.4602 mL | 4.9204 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4602 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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