| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Monomethyl auristatin E intermediate-2 itself does not directly target a biological receptor; it is a significant intermediate reactant in the multi-step chemical synthesis of MMAE. Once MMAE is synthesized, the final active drug targets tubulin, binding to the tubulin monomer to inhibit microtubule polymerization, thereby preventing mitosis and inducing apoptosis.
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| ln Vitro |
Not applicable. The intermediate-2 has no pharmacological activity of its own. Its utility is as a building block for MMAE synthesis. The final product, MMAE, is a highly potent tubulin inhibitor with low nanomolar cytotoxicity against a wide range of cancer cell lines. MMAE is extensively used as the cytotoxic component of ADCs.
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| ln Vivo |
Not applicable. The intermediate-2 is not administered to animals. ADCs that incorporate MMAE as the cytotoxic payload have demonstrated potent anti-tumor activity in preclinical xenograft models and have received regulatory approval for various cancers (e.g., brentuximab vedotin for Hodgkin lymphoma).
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| Enzyme Assay |
Not applicable. Monomethyl auristatin E intermediate-2 is a chemical synthesis intermediate, not a biological reagent. Its quality is assessed by chemical purity methods (HPLC, NMR, mass spectrometry) rather than biological assays. For chemical synthesis, it can be characterized by thin-layer chromatography (TLC) or LC-MS to confirm identity and purity.
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| Cell Assay |
Not applicable. The intermediate-2 is not used directly in cell-based assays. MMAE, the final ADC payload, is evaluated in cellular assays by treating cancer cell lines with MMAE or MMAE-containing ADCs (0.001-100 nM) for 72-120 hours, followed by viability assessment using MTT or CellTiter-Glo assays to determine IC50 values.
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| Animal Protocol |
Not applicable. The in vivo efficacy of MMAE-based ADCs is assessed in xenograft mouse models. ADCs are administered intravenously (e.g., 1-10 mg/kg, single or multiple doses), and tumor volume is measured over 2-6 weeks. The intermediate-2 itself is not used in animal studies.
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| ADME/Pharmacokinetics |
Monomethyl auristatin E intermediate-2 is a chemical intermediate with physicochemical properties defined by its structure. Detailed pharmacokinetic data is not provided for an intermediate. The final MMAE molecule has high potency and is primarily delivered as an ADC payload to target cells, with pharmacokinetics determined by the antibody component.
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| Toxicity/Toxicokinetics |
As a chemical intermediate, Monomethyl auristatin E intermediate-2 is handled with standard chemical safety precautions (gloves, goggles, fume hood). The final product MMAE is a highly potent cytotoxin with an LD50 in the low microg/kg range in animals, requiring special handling to avoid exposure. The intermediate itself is expected to be less toxic than MMAE but should still be handled with care.
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| References | |
| Additional Infomation |
Monomethyl auristatin E intermediate-2 is a research-grade chemical intermediate for ADC payload development. It is essential for the stepwise assembly of MMAE's complex structure and is ideal for researchers engaged in ADC payload synthesis, cytotoxic drug design, and structure-activity relationship (SAR) studies in oncology. This product is not for human use.
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| Molecular Formula |
C15H27NO6
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|---|---|
| Appearance |
White to off-white Solid-Liquid Mixture
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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, 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.) |
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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