| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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| ln Vitro |
In NCI-N87 cells, epertinib suppresses EGFR and HER2 phosphorylation with IC50 values of 4.5 and 1.6 nM, respectively [2]. With an IC50 of 26.5 nM, epertinib exhibits inhibitory effect against MDA-MB-361 cells[1]. A variety of cancer cell lines expressing EGFR and/or HER2 can be selectively inhibited from proliferating when exposed to epertinib (0–10 μM) for 72 hours [2].
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| ln Vivo |
Anti-tumor efficacy is demonstrated by epertinib (0-100 mg/kg), taken orally once day for 28 days [1]. Brain tumor growth is considerably decreased by epertinib (50 mg/kg, taken orally, once day for 30 days) [1]. In a dose-dependent way, epertinib (0-50 mg/kg) when taken orally once daily for 10–28 days considerably suppresses the growth of tumors [2].
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| Cell Assay |
Cell proliferation assay[2]
Cell Types: NCI-N87 (gastric), BT-474 (breast), SK-BR-3 (breast), MDA-MB-453 (breast), MDA-MB-175VII (breast), HT115 (colon), Calu-3 (lung), fR2 (breast) and MRC-5 (lung) Tested Concentrations: 0-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of growth of NCI-N87, BT-474, SK-BR -3. MDA-MB-453, MDA-MB-175VII, HT115, Calu-3, fR2 and MRC-5, IC50 values are 8.3 ± 2.6, 9.9 ± 0.8, 14.0 ± 3.6, 48.6 ± 3.1, 21.6±4.3, 53.3±8.6, 241.5±29.2, 5366.7±65.2 and 4964.6±340.3. |
| Animal Protocol |
Animal/Disease Models: Nude mice (BALB/cAJcl-nu/nu, intracranial implantation of MDA-MB-361 or BR2 cells) [1]
Doses: 12.5, 25, 50, 100 mg/kg Route of Administration: Orally, one time/day , lasted 28 days. Experimental Results: demonstrated antitumor activity in a mammary fat pad implantation model using both cell lines with comparable ED50 values (24.1 mg/kg for MDA-MB-361 and 26.5 mg/kg for BR2 (MDA- MB-361-luc-BR2) ), respectively). Animal/Disease Models: Nude mice (BALB/cAJcl-nu/nu, intracranial implantation of MDA-MB-361 or BR2 cells) [1] Doses: 50 mg/kg Route of Administration: Orally, one time/day for 30 days Experimental Results: The brain Dramatically diminished tumor volume, indicating that erpotinib can have potent anti-tumor activity in brain metastases even in the presence of an intact BTB (blood-tumor barrier). Animal/Disease Models: Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneously (sc) (sc) implanting human gastric cancer cell NCI-N87 cells on the back of nude mice) [2] Doses: 0, 6.25, 12.5, 25, 50 mg/kg Route of Administration: po (oral gavage), daily for 10-28 days Experimental Results: Dramatically inhibited the tumor growth in a dose-dependent manner. |
| References |
[1]. Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8(1):343.
[2]. Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8. |
| Molecular Formula |
C30H27CLFN5O3
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|---|---|
| Molecular Weight |
560.018489122391
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| Exact Mass |
559.178
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| CAS # |
908305-13-5
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| Related CAS # |
Epertinib hydrochloride;2071195-74-7
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| PubChem CID |
46701811
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
701.5±70.0 °C at 760 mmHg
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| Flash Point |
378.0±35.7 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.630
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| LogP |
6.09
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
40
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| Complexity |
899
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| Defined Atom Stereocenter Count |
1
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| SMILES |
N(C1C=CC(OCC2C=CC=C(F)C=2)=C(Cl)C=1)C1=NC=NC2=CC=C(C=C12)/C(/C#CC)=N/OC[C@@H]1NCCOC1
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| InChi Key |
IBCIAMOTBDGBJN-NRLRZRKLSA-N
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| InChi Code |
InChI=1S/C30H27ClFN5O3/c1-2-4-27(37-40-18-24-17-38-12-11-33-24)21-7-9-28-25(14-21)30(35-19-34-28)36-23-8-10-29(26(31)15-23)39-16-20-5-3-6-22(32)13-20/h3,5-10,13-15,19,24,33H,11-12,16-18H2,1H3,(H,34,35,36)/b37-27+/t24-/m1/s1
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| Chemical Name |
N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[(Z)-N-[[(3R)-morpholin-3-yl]methoxy]-C-prop-1-ynylcarbonimidoyl]quinazolin-4-amine
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 1.7857 mL | 8.9283 mL | 17.8565 mL | |
| 5 mM | 0.3571 mL | 1.7857 mL | 3.5713 mL | |
| 10 mM | 0.1786 mL | 0.8928 mL | 1.7857 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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