Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages.
Cancer Cell Int. 2023 Jul 2;23(1):129.
Exosome-derived circKIF20B suppresses gefitinib resistance and cell proliferation in non-small cell lung cancer
Gefitinib purchased from AbMole
Clin Transl Oncol. 2023 May;25(5):1425-1435.
ADAM12 promotes gemcitabine resistance by activating EGFR signaling pathway and induces EMT in bladder cancer
Gefitinib purchased from AbMole
Endocrinology. 2020 May 30;bqaa086.
RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice
Gefitinib purchased from AbMole
Clin Cancer Res. 2018 Nov 15;24(22):5658-5672.
Increased Synthesis of MCL-1 Protein Underlies Initial Survival of EGFR-Mutant Lung Cancer to EGFR Inhibitors and Provides a Novel Drug Target.
Gefitinib purchased from AbMole
Clin Cancer Res. 2018 Jan 1;24(1):197-208.
Epithelial-to-mesenchymal transition antagonizes response to targeted therapies in lung cancer by suppressing BIM
Gefitinib purchased from AbMole
Sci Rep. 2017 May 8;7(1):1578.
Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wallmediated lipolysis, inflammation and dysglycemia
Gefitinib purchased from AbMole
Cell Experiment | |
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Cell lines | MDA-361, SKBR-3, MDA-453 and BT-474 cells |
Preparation method | Monolayer Growth and Anchorage-independent Growth Assays. For monolayer growth, cells were seeded at a density of 3–4 104 cells in 12-well plates. Twenty-four h later, ZD1839 was added to the cells. Fresh medium ZD1839 was replaced on day 3. On day 5, cells were harvested by trypsinization and counted with a Zeiss Coulter Counter (Beckman Coulter, Miami, FL). Colony-forming assays in soft agarose were performed as described previously (30). Tumor cell colonies measuring 50 m were counted after 7 days using an Omnicon 3800 colony counter and Tumor Colony Analysis V2.IIA software (Imaging Products International, Inc.). |
Concentrations | 0.1–10 µ M |
Incubation time | 4 days |
Animal Experiment | |
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Animal models | BT-474 cells Xenograft in Athymic Mice |
Formulation | 0.05% Tween 80 |
Dosages | 200 mg/kg/day for 28 days |
Administration | oral gavage |
Molecular Weight | 446.90 |
Formula | C22H24ClFN4O3 |
CAS Number | 184475-35-2 |
Solubility (25°C) | DMSO 68 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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Almonertinib mesylate
Almonertinib mesylate is an orally active, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR sensitization and T790M resistance mutations, and also shows strong inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37, 0.29, and 0.21 nM, respectively. The IC50 of T790M/Del19 was 0.37, 0.29 and 0.21 nM, respectively, but the inhibitory effect on wild-type was weaker, with an IC50 of 3.39 nM. It can be used in the research of non-small cell lung cancer. |
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