| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
XQN70430 is a linker used in ADC technology. Its primary function is to connect a cytotoxic payload to a targeting antibody. The linker is designed to be specifically activated and cleaved in the tumor microenvironment, enabling the selective release of the drug at the target site. The MC-Ala-Ala-Asn(Trt)-PAB motif allows for site-specific conjugation and intracellular release of the payload after internalization into target cells. This targeted approach is crucial for reducing systemic toxicity and improving the therapeutic index of the drug.
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| ln Vitro |
In vitro, the activity of XQN70430 is assessed by evaluating its ability to conjugate cytotoxic drugs to antibodies and the subsequent release of the payload. The stability of the linker-drug conjugate in plasma and its specific cleavage by tumor-associated enzymes are key parameters measured to determine its functionality. The efficiency of the conjugation reaction and the purity of the resulting ADC are also critical quality attributes assessed in vitro.
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| ln Vivo |
In vivo activity is evaluated in xenograft mouse models bearing human tumors. The ADC constructed with XQN70430 is administered, and its antitumor efficacy is measured by tumor growth inhibition. The linker's ability to release the drug specifically in the tumor microenvironment, minimizing systemic toxicity, is a critical endpoint. The improved pharmacokinetic and pharmacodynamic profile of the ADC is also assessed in these models.
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| Enzyme Assay |
Assays to assess the functionality of XQN70430 focus on its ability to form stable conjugates. The maleimide group is reacted with thiol groups on an antibody, and the conjugation efficiency is measured, for example, by HPLC or mass spectrometry. The cleavage of the PAB spacer in the presence of tumor-relevant enzymes, such as cathepsin B, is monitored to confirm controlled drug release.
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| Cell Assay |
The in vitro cellular activity of the resulting ADC is evaluated in cancer cell lines. Cells are treated with the ADC, and cell viability is measured. The specificity and potency of the drug release are determined by comparing the effect on target-positive versus target-negative cells. The ADC's ability to be internalized and release the payload intracellularly is a key determinant of its activity.
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| Animal Protocol |
The in vivo efficacy of the ADC is assessed in mouse xenograft models. Tumor-bearing mice are treated with the ADC, and tumor growth is monitored. Pharmacodynamic markers of drug release and target engagement, such as changes in tumor cell proliferation or apoptosis, are also measured to confirm the mechanism of action.
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| ADME/Pharmacokinetics |
The pharmacokinetics of an ADC using XQN70430 is determined by measuring the concentration of the total antibody, the ADC, and the released payload in plasma over time. Parameters such as clearance, volume of distribution, and half-life are calculated to characterize the stability and exposure of the conjugate. A stable linker is essential for maintaining the ADC's integrity in circulation and delivering the payload to the tumor.
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| Toxicity/Toxicokinetics |
Toxicity studies evaluate the safety profile of the ADC. Parameters include body weight changes, clinical observations, and histopathological examination of tissues. The cleavable linker is designed to reduce off-target toxicity by ensuring drug release is confined to the tumor microenvironment. This targeted delivery is a key advantage of ADC technology.
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| Additional Infomation |
XQN70430 is a specialized tool for ADC development, enabling the targeted delivery of cytotoxic agents to tumor cells. Its design incorporates a cleavable moiety for controlled release, which is a key feature for improving the therapeutic index of ADCs. The compound was reported in patent WO 2016026458. Its versatility and efficacy make it a valuable tool in ADC technology and targeted drug delivery research.
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| Molecular Formula |
C46H50N6O8
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|---|---|
| Molecular Weight |
814.924611568451
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| Exact Mass |
814.369
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| Elemental Analysis |
C, 67.80; H, 6.18; N, 10.31; O, 15.71
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| CAS # |
1638970-43-0
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| PubChem CID |
130446078
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| Appearance |
Solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
60
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| Complexity |
1450
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)NC(C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)NC4=CC=C(C=C4)CO)NC(=O)CCCCCN5C(=O)C=CC5=O
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| InChi Key |
PRLBUJSXOZKWLC-QXGWMLRCSA-N
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| InChi Code |
InChI=1S/C46H50N6O8/c1-31(47-39(54)21-13-6-14-28-52-41(56)26-27-42(52)57)43(58)48-32(2)44(59)50-38(45(60)49-37-24-22-33(30-53)23-25-37)29-40(55)51-46(34-15-7-3-8-16-34,35-17-9-4-10-18-35)36-19-11-5-12-20-36/h3-5,7-12,15-20,22-27,31-32,38,53H,6,13-14,21,28-30H2,1-2H3,(H,47,54)(H,48,58)(H,49,60)(H,50,59)(H,51,55)/t31-,32-,38-/m0/s1
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| Chemical Name |
(S)-2-((S)-2-((S)-2-(7-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)heptanamido)propanamido)propanamido)-N1-(4-hydroxyphenyl)-N4-tritylsuccinamide
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| Synonyms |
XQN-70430XQN70430 XQN 70430 MC-Ala-Ala-Asn(Trt)-PAB
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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 | 1.2271 mL | 6.1356 mL | 12.2711 mL | |
| 5 mM | 0.2454 mL | 1.2271 mL | 2.4542 mL | |
| 10 mM | 0.1227 mL | 0.6136 mL | 1.2271 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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