| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| Targets |
Osimertinib Impurity C (Rezivertinib analogue 1) is structurally related to osimertinib, which targets mutant forms of the epidermal growth factor receptor (EGFR), particularly the T790M resistance mutation and activating EGFR mutations. As an analogue and process impurity, it may have similar but not identical target engagement properties. However, its specific target profile is not characterized in the available literature. It is primarily used as a reference standard and research tool for analytical method development and impurity profiling.
|
|---|---|
| ln Vitro |
In vitro, Osimertinib Impurity C is not typically evaluated for biological activity as it is an impurity rather than a therapeutic agent. It may be utilized in study/research of non-small cell lung cancer, but specific in vitro activity data are not reported. The compound serves primarily as a reference standard for analytical method development, quality control, and impurity profiling of osimertinib mesylate drug substance and drug products. Its biological activity, if any, would be expected to be similar to but potentially distinct from osimertinib.
|
| ln Vivo |
Specific in vivo data for Osimertinib Impurity C are not reported as the compound is not a therapeutic agent. It is a process impurity and research tool rather than a drug candidate. Any in vivo studies would be limited to toxicological evaluation of impurities in pharmaceutical development or to analytical method validation. The compound may be used in research on non-small cell lung cancer, but specific in vivo protocols are not available.
|
| Enzyme Assay |
The analytical characterization of Osimertinib Impurity C is performed using chromatographic methods such as HPLC and LC-MS. For identity confirmation, the compound is analyzed by mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy. Purity is assessed by HPLC with UV detection. The compound has a molecular formula of C₂₇H₃₃N₇O₂ and a molecular weight of 487.6 g/mol. It is soluble in DMSO at 50 mg/mL (102.54 mM) with heating.
|
| Cell Assay |
For cellular studies, Osimertinib Impurity C may be used in research on non-small cell lung cancer. However, specific cell-based assays for this impurity are not reported. If used in biological studies, the compound would typically be dissolved in DMSO and diluted in culture media at various concentrations. Cell viability would be assessed using MTT or similar assays in NSCLC cell lines. The compound is typically stored at -20°C.
|
| Animal Protocol |
In vivo studies for Osimertinib Impurity C are not typically conducted as it is an impurity rather than a therapeutic agent. If used in research, standard toxicology studies for pharmaceutical impurities would be performed according to ICH guidelines, including genotoxicity, repeat-dose toxicity, and carcinogenicity assessments as required for impurity qualification. However, specific protocols are not available.
|
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Osimertinib Impurity C are not reported. As a compound structurally related to osimertinib, it may have similar physicochemical properties but distinct PK characteristics. Pharmacokinetic studies would be required if the compound were to be evaluated as a potential drug candidate, but as an impurity, such studies are not typically performed. The compound is soluble in DMSO at 50 mg/mL.
|
| Toxicity/Toxicokinetics |
As a process impurity in osimertinib mesylate, the toxicological profile of Osimertinib Impurity C would be evaluated as part of the overall impurity qualification strategy for the drug substance. The compound is typically present at low levels (<0.15% by HPLC), and its toxicity at these levels is considered acceptable based on ICH guidelines for drug impurities. The compound should be handled with appropriate safety precautions as it is a chemical research standard.
|
| References | |
| Additional Infomation |
Osimertinib Impurity C (Rezivertinib analogue 1) is a process impurity in osimertinib mesylate used for NSCLC research. Molecular formula: C₂₇H₃₃N₇O₂, MW: 487.6. Soluble in DMSO at 50 mg/mL. No clinical applications exist. For research use only as an analytical reference standard.
|
| Molecular Formula |
C27H33N7O2
|
|---|---|
| Molecular Weight |
487.596625089645
|
| Exact Mass |
487.269
|
| CAS # |
2227103-37-7
|
| PubChem CID |
141514457
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
3.1
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
36
|
| Complexity |
710
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1C2=CC=CC=C2C(C2C=CN=C(NC3C=C(NC(=O)C)C(N(C)CCN(C)C)=CC=3OC)N=2)=C1
|
| InChi Key |
FZPRMSLRRIEUNO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C27H33N7O2/c1-18(35)29-22-15-23(26(36-6)16-25(22)33(4)14-13-32(2)3)31-27-28-12-11-21(30-27)20-17-34(5)24-10-8-7-9-19(20)24/h7-12,15-17H,13-14H2,1-6H3,(H,29,35)(H,28,30,31)
|
| Chemical Name |
N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]acetamide
|
| 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) |
DMSO : ~50 mg/mL (~102.54 mM)
|
|---|---|
| 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 | 2.0509 mL | 10.2543 mL | 20.5086 mL | |
| 5 mM | 0.4102 mL | 2.0509 mL | 4.1017 mL | |
| 10 mM | 0.2051 mL | 1.0254 mL | 2.0509 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
