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ln Vitro |
The suppression of two neuregulin-1 (NRG1) rearranged fusion cell lines (MDA-MB-175-VII, DOC4-NRG1 fusion, and LUAD-0061AS3, SLC3A2-NRG1 fusion) by seribantumab (0.1 nmol/L-10 μmol/L; 96 h) is dose-dependent. The IC50 values for suppressing MDA-MB-175-VII, LUAD-0061AS3, MCF-7, and HBECp53 cells were, respectively, 0.02, 1.4, 45.2, and 203 μmol/L[1]. Effective growth inhibition of NRG1 fusion or NRG1 amplified tumor cell lines is achieved by seribantumab (0.1, 1 and 10 μmol/L; 24-48 h) [1]. Strong growth inhibition of NRG1-b1-stimulated MCF-7 cells is seen upon treatment with seribantumab (0-0.5 μmol/L; 96 h) [1]. Apoptosis is induced in NRG1-rearranged cells by seribantumab (0-10 μmol/L; 48 h) [1]. Phosphorylation of NRG1 downstream regulators is inhibited by seribantumab (0-10 μmol/L; 1 h) [1].
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ln Vivo |
Seribantumab (0.6–1 mg; i.p. every two weeks for a co-injection) inhibits the growth of tumors arising from non-small cell lung cancer more effectively than afatinib, while also promoting the production of apoptotic markers and phosphorylating growth regulatory factors[1]. In a mouse model of high-grade serous ovarian cancer (HGSOC), seribantumab (1–10 mg; i.p. once every two weeks) substantially reduces tumor cell burden without appreciably altering animal weight or health [1].
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Cell Assay |
Apoptosis Analysis[1]
Cell Types: MDA-MB-175-VII and LUAD-0061AS3 cell lines Tested Concentrations: 0-10 μmol/L Incubation Duration: 48 hrs (hours) Experimental Results: Dose-dependently increased caspase 3/7 activity and induced apoptosis of NRG1 fusion-positive breast and lung cancer cell lines. Western Blot Analysis[1] Cell Types: LUAD-0061AS3 and HBECp53-CD74-NRG1 cell lines Tested Concentrations: 0, 0.001, 0.01, 0.1, 1 and 10 μmol/L Incubation Duration: 1 hour Experimental Results: Inhibited the phosphorylation of EGFR, HER2, HER3, HER4, AKT and STAT3 in LUAD-0061AS3 cells. Completely inhibited HER3, AKT, p70S6K and STAT3, and decreased phosphorylation of HER2, EGFR and HER4 to a lesser extent in HBECp53-CD74-NRG1 cells. |
Animal Protocol |
Animal/Disease Models: Immunocompromised mice with LUAD-0061AS3 PDX tumors implanted[1]
Doses: 0.6, 0.75 and 1 mg Route of Administration: intraperitoneal (ip)injection; 0.6, 0.75 and 1 mg for once Experimental Results: Effectively diminished tumor growth of mice and time- and dose-dependently diminished phosphorylation of HER2, HER3, AKT, and ERK1/2. Induced the expression if proapoptotic protein, BIM. |
References |
[1]. Odintsov I, et al. The Anti-HER3 mAb Seribantumab Effectively Inhibits Growth of Patient-Derived and Isogenic Cell Line and Xenograft Models with Oncogenic NRG1 Fusions. Clin Cancer Res. 2021 Jun 1;27(11):3154-3166.
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Molecular Weight |
143.2 (kDa)
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CAS # |
1334296-12-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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.) |
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.