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CAS No. : 1638281-44-3
MCE 国际站:Osimertinib-d6
产品活性:Osimertinib-d6 是氘标记的 Osimtinib。 Osimtinib 是一种共价结合、具有口服活性、不可逆和突变的选择性的 EGFR 抑制剂,其有效抑制 L858R (IC50=12 nM) 和 L858R/T790M (IC50=1 nM) EGFR。Osimtinib 解决了肺癌 T790M 突变介导的 EGFR 抑制剂耐药。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively.
Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively.
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16-701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells) .
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50 of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50 of 650 and 461 nM in Calu3 and H2073 respectively).
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rate of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) .
In Vivo: Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
相关产品:EGFR/HER2/CDK9-IN-2 | Lapatinib ditosylate | BMS-690514 | Erlotinib-d6 hydrochloride | EGFR/CDK2-IN-1 | JBJ-04-125-02 | EGFR-IN-22 | EGFR-IN-34 | Epertinib | Ponezumab | Erlotinib Hydrochloride | EGFR-IN-36 | EGFR-IN-62 | Genistein | Panitumumab (anti-EGFR) | Lirafugratinib | Lapatinib-d7 dihydrochloride | (E/Z)-CP-724714 | TAS0728 | Rezivertinib | Tucatinib hemiethanolate | Osimertinib mesylate | AV-412 free base | Falnidamol | EGFR/ErbB-2/ErbB-4 inhibitor-2 | Trastuzumab | EGFR-IN-58 | Naquotinib | MS9449
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