Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity in H1975 cells and the mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.
説明 | EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity in H1975 cells and the mutant HCC827 cells with IC50s of 4 and 28 nM, respectively. |
ターゲット&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]. |
分子量 | 551.04 |
分子式 | C28H31ClN6O4 |
CAS No. | 2227455-78-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (18.15 mM)
You can also refer to dose conversion for different animals. 詳細
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EGFR-IN-1 hydrochloride 2227455-78-7 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR EGFR-IN-1 Hydrochloride EGFRIN1 hydrochloride EGFR IN 1 hydrochloride Inhibitor inhibitor inhibit