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EGFR-IN-1 hydrochloride
🥰Excellent
Catalog No. T11157LCas No. 2227455-78-7
EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.
EGFR-IN-1 hydrochloride
🥰Excellent
Purity: 99.8%
Catalog No. T11157LCas No. 2227455-78-7
EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | 56 € | In Stock | |
| 5 mg | 145 € | In Stock | |
| 10 mg | 215 € | In Stock | |
| 25 mg | 337 € | In Stock | |
| 50 mg | 452 € | In Stock | |
| 100 mg | 620 € | In Stock | |
| 200 mg | 838 € | In Stock | |
| 1 mL x 10 mM (in DMSO) | 201 € | In Stock |
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Purity:99.8%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively. |
| Targets&IC50 | p-EGFR:4-9nM |
| In vitro | EGFR-IN-1 is highly selective against a panel of 100 kinases and inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively[1]. |
| In vivo | In female athymic nude mice with H1975 Tumor Xenograft, gavage administration of EGFR-IN-1 hydrochloride (30 mg/kg) significantly inhibits the tumor growth without observed loss in body weight. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR and a systemic exposure (AUC0-inf.) of 0.33 μM. h[1]. |
| Molecular Weight | 551.04 |
| Formula | C28H31ClN6O4 |
| Cas No. | 2227455-78-7 |
| Smiles | Cl.O=C(C=C)NC1=CC=CC(=C1)N2C(=O)C=C(C=3C=NC(=NC32)NC4=CC=C(OCCN(C)C)C=C4OC)C |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (18.15 mM)  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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