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CAS No. :
MCE 国际站:EGFR T790M/L858R-IN-2
产品活性:EGFRT790M/L858R-IN-2 是一种有效的选择性 EGFRT790M/L858R 抑制剂,对 EGFRT790M/L858R 和 EGFR WT 的 IC50 值分别为 3.5, 1290 nM。EGFRT790M/L858R-IN-2 降低 p-EGFR、P-AKT、P-ERK1/2 的表达。EGFRT790M/L858R-IN-2 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G1 期。EGFRT790M/L858R-IN-2 具有抗癌活性。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK | Apoptosis
作用靶点:EGFR | Apoptosis
In Vitro: EGFRT790M/L858R-IN-2 (compound 28f) (0.1, 1, 10 µM; 4 h) decreases the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells.
EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 48 h) induces apoptosis and cell cycle arrest in the G1 phase in H1975, HCC827 cells.
EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 14 days) inhibits colony formation and cell migration in a dose-dependent manner.
In Vivo: EGFRT790M/L858R-IN-2 (5, 10, 20 mg/kg; i.p.; daily) inhibits tumor growth in a dose-dependent manner.
Pharmacokinetic Parameters of EGFRT790M/L858R-IN-2 in Male Sprague-Dawley rats.
parameter |
i.v. (1 mg/kg) |
T1/2 (h) |
1.76 ± 0.65 |
Cmax (ng/mL) |
649.90 ± 54.71 |
AUC0-t (h*ng/ml) |
1036.86 ± 137.03 |
AUC0–∞ (h ng/ml) |
1048.74 ± 134.39 |
Vz (mL/kg) |
2515.40 ± 1184.92 |
CL(mL/min/kg) |
16.07 ± 2.06 |
Male Sprague-Dawley rats, 1 mg/kg iv
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