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250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
When mipasetamab uzoptirine binds to both soluble and membrane AXL, tumor cells that express AXL internalize it and release PBD dimers, which cause DNA interstrand cross-linking and eventual cell death [1]. AXL-positive human cancer cells (Panc-1, A-172, SK-LU-1, MDA-MB-231, SK-OV-3, NCI-H1299, SN12C) are specifically inhibited from growing by dipasetamab uzoptirine [1]. Mipasetamab uzoptirine (0 hours, 4°C) exhibits robust binding to the cell surface in SN12C cells and lysosome colocalization at 1 hour [1]. In SN12C cells, the amount of DNA interstrand cross-links is increased by dipastetamab uzoptirine [1].
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ln Vivo |
Mipasetamab uzoptirine (0.3-1 mg/kg, intravenously) inhibits tumor growth in MDA-MB-231 TNBC xenograft and SN12C xenograft mouse models[1]. Mipasetamab uzoptirine (6 mg/kg, intravenously) is well tolerated and exhibits excellent stability in rats[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Panc-1, A-172, SK-LU-1, MDA-MB-231, SK-OV-3, NCI-H1299, and SN12C Tested Concentrations: 0-20 nM approximately Incubation Duration: 5-8 days Experimental Results: Inhibited cell growth with IC50s of 0.47, 0.59, 0.02, 0.35, 0.11, 2.2, 0.83, 9.29, 14.62 nM respectively. |
Animal Protocol |
Animal/Disease Models: SN12C xenograft mice model[1].
Doses: 0.3-1 mg/kg Route of Administration: iv Experimental Results: Inhibited tumor growth and increased survival rate. |
References |
[1]. Zammarchi F, et al. Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody-drug Conjugate Targeting AXL-expressing Cancers. Mol Cancer Ther. 2022 Apr 1;21(4):582-593.
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CAS # |
2304799-73-1
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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.) |
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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.