| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Mc-Val-Cit-Pab-Gefitinib chloride targets the epidermal growth factor receptor (EGFR) tyrosine kinase via the Gefitinib payload. The Mc-Val-Cit-PAB linker is a cathepsin-cleavable peptide sequence (Val-Cit) designed for intracellular release following ADC internalization.
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|---|---|
| ln Vitro |
Not available. As an ADC drug-linker conjugate, its in vitro activity is assessed when conjugated to an antibody. Free Gefitinib potently inhibits EGFR kinase activity with IC50 values in the low nanomolar range (typically 10-100 nM) in biochemical assays and EGFR-dependent cancer cell proliferation.
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| ln Vivo |
Not available. The in vivo activity of Mc-Val-Cit-Pab-Gefitinib chloride as an ADC conjugate would be evaluated in xenograft mouse models bearing EGFR-expressing human tumors, assessing tumor growth inhibition, survival extension, and target engagement at doses typically ranging from 1-10 mg/kg.
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| Enzyme Assay |
Not available. For ADC linker-payload evaluation, standard in vitro protocols involve cathepsin B cleavage assays where the linker conjugate is incubated with recombinant cathepsin B (10-100 nM) at 37degC, and release of Gefitinib is quantified by HPLC-MS at various time points.
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| Cell Assay |
Not available. For ADC activity assessment, typical cellular protocols involve treating EGFR-positive cancer cells (e.g., A431, HCC827) with the ADC conjugate (0.001-10 nM) for 72-120 hours, followed by cell viability assessment using MTT or CellTiter-Glo assays.
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| Animal Protocol |
Not available. For in vivo evaluation of ADCs containing this linker-payload, standard protocols involve intravenous administration of the ADC conjugate (1-30 mg/kg, q7d or q14d) in tumor-bearing mice, with monitoring of tumor volume, body weight, and survival over 4-6 weeks.
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| ADME/Pharmacokinetics |
Not available. The Mc-Val-Cit-PAB linker is designed for serum stability with intracellular release via cathepsin proteases. This cleavage mechanism typically provides good pharmacokinetic properties with prolonged circulation half-life when conjugated to antibodies.
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| Toxicity/Toxicokinetics |
Not available. The toxicity profile of Mc-Val-Cit-Pab-Gefitinib chloride would be determined by the conjugated antibody specificity. Common ADC-related toxicities include off-target effects, thrombocytopenia, and hepatotoxicity, but specific data for this conjugate are not reported.
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| References | |
| Additional Infomation |
Mc-Val-Cit-Pab-Gefitinib chloride is a research-grade ADC drug-linker conjugate designed for targeted cancer therapy development. It has not undergone clinical trials nor received regulatory approval for any indication. This product is strictly for research use in ADC development and evaluation of EGFR-targeted therapies.
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| Molecular Formula |
C50H63CL2FN10O9
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|---|---|
| Molecular Weight |
1038.00
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| Appearance |
White to off-white solid powder
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| SMILES |
COC1=CC2=C(C=C1OCCCN3CCOCC3)C(NC(C=C4)=CC(Cl)=C4F)=NC=[N+]2CC(C=C5)=CC=C5NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(CCCCCN(C6=O)C(C=C6)=O)=O)=O)=O.[Cl-]
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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 and light. |
| 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) |
DMSO: ~50 mg/mL (~48.2 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (1.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 1.25 mg/mL (1.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9634 mL | 4.8170 mL | 9.6339 mL | |
| 5 mM | 0.1927 mL | 0.9634 mL | 1.9268 mL | |
| 10 mM | 0.0963 mL | 0.4817 mL | 0.9634 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.
Products are for research use only; We do not sell to patients
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