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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
Aprutumab ixadotin (0.097–0.83 nM; 72 hours) showed an antigen-binding affinity of 0.29 nM for FGFR2 and exhibited inhibitory activity in various cell lines with an IC50 of 0.097–0.83 nM [1]. Aprutumab ixadotin specifically induced apoptosis in FGFR2-positive cells (SUN-52PE, SUN-16) in vitro [1].
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| ln Vivo |
Aprutumab ixadotin (5 mg/kg and 7.5 mg/kg; intravenous injection; once a week for 30 days) was well tolerated and caused partial tumor regression in mouse SNU-16, MFM-223 or NCI-H716 xenograft models [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: SNU-16, KATO III, SUM-52PE, NCI-H716 and MFM-223 cells; MDA-MB-231 cells; KYSE-180 cells; 4T1 cells Tested Concentrations: 0.097-0.83 nM Incubation Duration: 72 hours Experimental Results: Inhibited cell viability. |
| Animal Protocol |
Animal/Disease Models: SNU-16 xenograft model in female NOD scid mice and MFM-223 and NCI-H716 xenograft models in female NMRI nu/nu mice [1]
Doses: 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 7.5 mg/kg, 15 mg/kg Route of Administration: Intravenous injection; once a week for 4 weeks Experimental Results: In the SNU-16 xenograft model, tumor growth was significantly reduced by at least 90% in the 5 mg/kg dose group. However, tumor growth was not significantly inhibited in the 0.5 mg/kg or 1 mg/kg dose groups compared with the solvent control group. In the MFM-223 model, tumor volume was significantly reduced in the 1 mg/kg and 5 mg/kg dose groups. In a cell line-derived xenograft model overexpressing FGFR2 (NCI-H716 human colorectal cancer model), a dose of 7.5 mg/kg significantly inhibited tumor growth. |
| References |
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| Molecular Formula |
C57H95N9O11
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|---|---|
| Molecular Weight |
1082.41791558266
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| CAS # |
1708947-48-1
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| Appearance |
Colorless to light yellow liquid
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| SMILES |
[Aprutumab ixadotin]
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| Synonyms |
BAY 1187982
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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 | 0.9239 mL | 4.6193 mL | 9.2386 mL | |
| 5 mM | 0.1848 mL | 0.9239 mL | 1.8477 mL | |
| 10 mM | 0.0924 mL | 0.4619 mL | 0.9239 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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