| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Mutant epidermal growth factor receptor (EGFR), including L858R, Exon 19 deletion, and T790M resistance mutants.
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|---|---|
| ln Vitro |
INVIVO3627 selectively inhibits mutant EGFR isoforms (L858R, Exon 19 deletion, T790M). Detailed IC50 values for each mutant and selectivity over wild-type EGFR are available in primary research publications. The compound inhibits EGFR kinase activity, blocking downstream signaling pathways such as PI3K/AKT and MAPK/ERK.
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| ln Vivo |
INVIVO3627 inhibits the growth of EGFR-mutant cancer cell lines by blocking EGFR kinase activity and downstream signaling. It induces cell cycle arrest and apoptosis in cells harboring EGFR mutations. The compound shows selectivity for mutant EGFR over wild-type EGFR, potentially reducing on-target toxicities associated with wild-type EGFR inhibition.
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| Enzyme Assay |
EGFR kinase activity is measured using kinase assay kits with synthetic peptide substrates or ATP competition assays. Recombinant wild-type and mutant EGFR proteins are incubated with ATP, substrate, and varying concentrations of INVIVO3627. Phosphorylation of substrate is detected by radioactivity, fluorescence, or ELISA to determine IC50 values.
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| Cell Assay |
EGFR-mutant cancer cell lines (e.g., HCC827 with Exon 19 deletion, H1975 with L858R/T790M) are treated with INVIVO3627 at various concentrations. Cell viability is assessed by MTT or CellTiter-Glo assays. EGFR phosphorylation and downstream signaling are evaluated by Western blot. Apoptosis and cell cycle distribution are assessed by flow cytometry.
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| Animal Protocol |
INVIVO3627 is evaluated in mouse xenograft models of EGFR-mutant NSCLC. Tumor-bearing mice are treated with INVIVO3627 via oral or intraperitoneal administration. Tumor growth inhibition, EGFR phosphorylation, and survival are monitored.
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| ADME/Pharmacokinetics |
INVIVO3627 has molecular weight 520.03 and formula C27H30ClN7O2. It is a small-molecule EGFR inhibitor suitable for oral administration. Detailed PK parameters (half-life, bioavailability, clearance) are available in primary research publications.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for INVIVO3627 are limited. As a mutant-selective EGFR inhibitor, it may have a better safety profile compared to first-generation EGFR inhibitors due to reduced wild-type EGFR inhibition.
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| References | |
| Additional Infomation |
INVIVO3627 is a research tool for studying EGFR-mutant cancers and resistance mechanisms. Its mechanism involves selective inhibition of mutant EGFR kinase activity, blocking oncogenic signaling in EGFR-mutant tumors. No clinical trials or approved indications exist.
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| Molecular Formula |
C27H30CLN7O2
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|---|---|
| Molecular Weight |
520.034
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| Exact Mass |
519.215
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| CAS # |
1421373-62-7
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| PubChem CID |
78357783
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.298
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
37
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| Complexity |
758
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCN(C)C1=CC(=C(C=C1NC(=O)C=C)NC2=NC=C(C(=N2)C3=CNC4=CC=CC=C43)Cl)OC
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| InChi Key |
SUPQPCQJBYPRPC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H30ClN7O2/c1-6-25(36)31-21-13-22(24(37-5)14-23(21)35(4)12-11-34(2)3)32-27-30-16-19(28)26(33-27)18-15-29-20-10-8-7-9-17(18)20/h6-10,13-16,29H,1,11-12H2,2-5H3,(H,31,36)(H,30,32,33)
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| Chemical Name |
N-[5-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-2-[2-(dimethylamino)ethyl-methylamino]-4-methoxyphenyl]prop-2-enamide
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| Synonyms |
INVIVO-3627; INVIVO 3627; INVIVO3627
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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) |
DMSO : ≥ 50 mg/mL (~96.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.81 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 25.0 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: ≥ 2.5 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9230 mL | 9.6148 mL | 19.2297 mL | |
| 5 mM | 0.3846 mL | 1.9230 mL | 3.8459 mL | |
| 10 mM | 0.1923 mL | 0.9615 mL | 1.9230 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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