| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
EGFR[2]
Epitinib succinate targets the epidermal growth factor receptor (EGFR). It is a selective EGFR-TKI designed for maximum brain penetration. Upon administration, epitinib inhibits the activity of EGFR, thereby preventing EGFR-mediated signaling. This may lead to induction of cell death and inhibition of tumor growth in EGFR-overexpressing tumor cells. |
|---|---|
| ln Vitro |
A selective and potent oral epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) for maximum brain penetration is called epitinib succinate[1][2].
In vitro, Epitinib succinate has been shown to be a potent and selective EGFR inhibitor. Its activity is assessed using kinase assays and cell-based proliferation assays in EGFR-overexpressing cancer cell lines. These studies confirm its potential as a therapeutic agent for cancers with EGFR overexpression. |
| ln Vivo |
In vivo, Epitinib succinate has been studied in animal models of cancer, particularly those involving brain metastases due to its BBB-penetrating properties. Its ability to cross the blood-brain barrier is a key feature for the treatment of central nervous system tumors.
|
| Enzyme Assay |
Cell-free assays for Epitinib succinate typically involve measuring its inhibitory activity against EGFR kinase using biochemical kinase assays. The compound's IC50 value is determined by measuring the phosphorylation of a substrate in the presence of varying concentrations of the inhibitor. These assays are used to characterize the compound's potency and selectivity.
|
| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Epitinib succinate. EGFR-overexpressing cancer cell lines are treated with the compound. Cell viability and proliferation are measured to assess the compound's anti-proliferative effects. EGFR phosphorylation is also measured to confirm inhibition of the target kinase.
|
| Animal Protocol |
In vivo animal experiments typically involve xenograft models of EGFR-driven cancers, including those with brain metastases. Mice bearing these tumors are administered Epitinib succinate orally. Tumor growth is monitored over time to assess the compound's efficacy.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Epitinib succinate are characterized by its oral bioavailability and ability to penetrate the blood-brain barrier. Its molecular formula is C28H32N6O6, and it has a molecular weight of 548.59. The succinate salt form enhances its solubility and stability.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Epitinib succinate is likely consistent with other EGFR TKIs. Common adverse effects may include diarrhea, skin rash, and fatigue. Its ability to penetrate the BBB may also lead to central nervous system-related side effects. Preclinical studies support its safety profile.
|
| References |
|
| Additional Infomation |
Epitinib succinate is the succinate form of Epitinib, an oral epidermal growth factor receptor (EGFR) inhibitor with potential antitumor activity. After administration, Epitinib inhibits EGFR activity, thereby blocking EGFR-mediated signaling. This may lead to cell death and tumor growth inhibition in EGFR-overexpressing tumor cells. EGFR is a receptor tyrosine kinase (RTK) that is overexpressed in certain tumor types and plays a crucial role in tumor cell proliferation and angiogenesis.
Epitinib succinate is a selective EGFR-TKI being developed for the treatment of cancers with EGFR overexpression, particularly those with brain metastases. Its ability to penetrate the blood-brain barrier is a key feature. The compound is in clinical development for the treatment of non-small cell lung cancer and other solid tumors. |
| Molecular Formula |
C28H32N6O6
|
|---|---|
| Molecular Weight |
548.590286254883
|
| Exact Mass |
548.238
|
| CAS # |
2252334-12-4
|
| Related CAS # |
Epitinib;1203902-67-3
|
| PubChem CID |
135379897
|
| Appearance |
White to light yellow solid powder
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
40
|
| Complexity |
765
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(NC1C(=CC2C(=C(N=CN=2)NC2C=CC=C(C#C)C=2)C=1)OC)N1CCN(CC)CC1.OC(CCC(=O)O)=O
|
| InChi Key |
HISXHQFAOANCJX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H26N6O2.C4H6O4/c1-4-17-7-6-8-18(13-17)27-23-19-14-21(22(32-3)15-20(19)25-16-26-23)28-24(31)30-11-9-29(5-2)10-12-30;5-3(6)1-2-4(7)8/h1,6-8,13-16H,5,9-12H2,2-3H3,(H,28,31)(H,25,26,27);1-2H2,(H,5,6)(H,7,8)
|
| Chemical Name |
butanedioic acid;4-ethyl-N-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]piperazine-1-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 12.5 mg/mL (22.79 mM)
H2O: 1 mg/mL (1.82 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (2.28 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 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8229 mL | 9.1143 mL | 18.2285 mL | |
| 5 mM | 0.3646 mL | 1.8229 mL | 3.6457 mL | |
| 10 mM | 0.1823 mL | 0.9114 mL | 1.8229 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.
Link: https://clinicaltrials.gov/ct2/show/NCT03231501
Conditions:GlioblastomaProducts are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
