| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The IC50 values of EGFR-IN-169 (Compound 4e) against HCT-116 cells were 4.46 μM, against CT-26 cells 6.89 μM, against HT-29 cells 9.03 μM, against SW620 cells 16.01 μM, and against Caco-2 cells 18.98 μM[1]. EGFR-IN-169 (5-10 μM, 48 h) inhibited colony formation in HCT-116 and CT-26 cell lines[1]. EGFR-IN-169 (2.5-10 μM, 48 h) induced significant G0/G1 phase arrest in HCT-116 cells[1]. EGFR-IN-169 (2.5-10 μM, 24-48 h) induced apoptosis in HCT-116 cells[1]. EGFR-IN-169 (2.5-10 μM, 12 h) can induce mitochondrial damage and reactive oxygen species (ROS) accumulation in HCT-116 cells[1]. EGFR-IN-169 (5 μM, 48 h) can inhibit the migration and invasion of HCT-116 cells[1]. EGFR-IN-169 (2.5-10 μM) can inhibit the activation of RalA protein in HCT-116 cells in a dose-dependent manner[1].
|
|---|---|
| ln Vivo |
EGFR-IN-169 (Compound 4e) (100 mg/kg, once daily for 7–14 days) showed good safety in mice[1]. EGFR-IN-169 (5–10 mg/kg, intraperitoneal injection) blocked tumor growth in the CT-26 tumor model[1].
|
| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: HCT-116 cells Tested Concentrations: 2.5, 5 and 10 μM Incubation Duration: 48 h Experimental Results: Induced significant G0/G1 phase arrest. Decreased cells in the S phase and G2/M phase. Downregulated the expression of CDK2, CDK4, CDK6, and Cyclin D1. Apoptosis Analysis[1] Cell Types: HCT-116 cells Tested Concentrations: 2.5, 5 and 10 μM Incubation Duration: 24 and 48 h Experimental Results: Enhanced membrane permeability and promoted a time-dependent shift from early to late apoptosis. Reduced Bcl-2 levels and increased Bax levels. Increased γ-H2AX expression. |
| Animal Protocol |
Animal/Disease Models: CT-26 tumor mice models[1]
Doses: 5 and 10 mg/kg Route of Administration: Intraperitoneally injection Experimental Results: Significantly reduced tumor weight. Had no effect on body weight. Showed a significantly reduced proportion of proliferative marker Ki-67. |
| References |
| Molecular Formula |
C40H56CLNO6
|
|---|---|
| Molecular Weight |
682.33
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 1.4656 mL | 7.3278 mL | 14.6557 mL | |
| 5 mM | 0.2931 mL | 1.4656 mL | 2.9311 mL | |
| 10 mM | 0.1466 mL | 0.7328 mL | 1.4656 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
