| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
Purity: =100%
| Targets |
6-Maleimidocaproic acid hydrazide TFA does not have a specific biological target as a therapeutic agent. It is a bioconjugation reagent designed to crosslink biomolecules by reacting with sulfhydryl groups on proteins and carbonyl groups on carbohydrates or oxidized antibodies. The maleimide group forms stable thioether bonds with thiol-containing biomolecules, while the hydrazide group reacts with aldehydes or ketones to form hydrazones.
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|---|---|
| ln Vitro |
The compound is a chemical reagent and does not possess intrinsic biological activity. Its in vitro applications include the preparation of antibody-drug conjugates (ADCs), immunoconjugates, and protein-protein conjugates. It has been used in studies of albumin-binding prodrugs of doxorubicin that are cleaved by cathepsin B. The compound enables the covalent attachment of therapeutic payloads to targeting antibodies or carrier proteins.
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| ln Vivo |
The compound is not intended for in vivo use as a therapeutic agent. It is a research reagent used for the synthesis of bioconjugates that may subsequently be evaluated in vivo. No direct in vivo activity data are available for this compound itself.
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| Enzyme Assay |
6-Maleimidocaproic acid hydrazide TFA is a chemical crosslinker and is not used in enzyme/receptor binding assays. Typical non-cell-based applications involve conjugation reactions in aqueous buffers at pH 6.5-7.5 for maleimide-thiol coupling. The hydrazide group reacts with carbonyls under mildly acidic conditions (pH 5-6) to form hydrazone linkages. The compound is dissolved in DMSO or DMF prior to addition to protein solutions.
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| Cell Assay |
No specific cell-based assay protocols are available for this compound. It is used in vitro for the chemical modification of proteins and peptides, which may subsequently be tested in cellular assays. The compound itself is not applied directly to cells due to its reactive nature.
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| Animal Protocol |
No in vivo animal experiment protocols are applicable for 6-Maleimidocaproic acid hydrazide TFA itself. The compound is used in the synthesis of bioconjugates that may be tested in animal models. However, the crosslinker itself is not administered to animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic data are not applicable for 6-Maleimidocaproic acid hydrazide TFA. As a chemical crosslinking reagent, it is not intended for systemic administration. The compound is used in vitro for bioconjugation purposes.
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| Toxicity/Toxicokinetics |
Toxicological data are limited. The compound is a reactive chemical and may cause irritation upon contact with skin, eyes, or mucous membranes. Standard laboratory safety precautions should be followed when handling the compound. It is for research use only and is not for human or veterinary use.
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| References |
[1]. Khalid Abu Ajaj, et al. In vitro and in vivo study of an albumin-binding prodrug of doxorubicin that is cleaved by cathepsin B. Cancer Chemother Pharmacol. 2009 Jul;64(2):413-8.
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| Additional Infomation |
6-Maleimidocaproic acid hydrazide TFA (EMCH-TFA) is a heterobifunctional crosslinking reagent containing a maleimide group for thiol-selective conjugation and a hydrazide group for carbonyl-reactive coupling. It is used in the preparation of immunoconjugates, antibody-drug conjugates, and albumin-binding prodrugs. The compound is a research chemical and has no clinical approvals or applications.
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| Molecular Formula |
C12H16F3N3O5
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|---|---|
| Molecular Weight |
339.27
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| Exact Mass |
339.104
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| CAS # |
151038-94-7
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| PubChem CID |
23509306
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| Appearance |
Typically exists as solid at room temperature
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| Melting Point |
104-105ºC
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| LogP |
1.124
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
391
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C(=O)O[H])(F)F.O=C1C([H])=C([H])C(N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(N([H])N([H])[H])=O)=O
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| InChi Key |
DRURMGRBAVYWCL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15N3O3.C2HF3O2/c11-12-8(14)4-2-1-3-7-13-9(15)5-6-10(13)16;3-2(4,5)1(6)7/h5-6H,1-4,7,11H2,(H,12,14);(H,6,7)
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| Chemical Name |
6-(2,5-dioxopyrrol-1-yl)hexanehydrazide;2,2,2-trifluoroacetic 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 |
| 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 | 2.9475 mL | 14.7375 mL | 29.4750 mL | |
| 5 mM | 0.5895 mL | 2.9475 mL | 5.8950 mL | |
| 10 mM | 0.2948 mL | 1.4738 mL | 2.9475 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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