Osimertinib (GMP)
Osimertinib (AZD-9291; Mereletinib) GMP is the GMP level of Osimertinib (HY-15772). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Osimertinib GMP is an inhibitor that selectively targets EGFRT790M and activated EGFR mutants. Osimertinib GMP exerts multiple anti-tumor mechanisms, including radiosensitization, induction of apoptosis and ferroptosis, as well as inhibition of cancer stemness. Osimertinib GMP suppresses EGFR nuclear translocation and downstream survival signaling pathways, significantly reduces cell viability and lipid droplet content, and also exerts synergistic effects with radiotherapy or specific targeted agents to effectively overcome drug resistance and radioresistance. Formulations of Osimertinib GMP modified with liposomes or iRGD enable sustained release, tumor-specific accumulation, and breakthrough of the blood-brain barrier limitation. Osimertinib GMP can be used in research related to radioresistant glioblastoma and non-small cell lung cancer.
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- CAS 番号: 1421373-65-0
- 分子式: C28H33N7O2
- 分子量:499.61
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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EGFRL858R/T790M |
Combination GMP with Osimertinib (500-2500 nM; 72 h) and Ganetespib (HY-15205) or Luminespib (HY-10215) enhances the inhibitory effect on cell viability of Osimertinib (HY-15772)-resistant non-small cell lung cancer cell lines PC9-OR2 and PC9-OR4, as well as the parental PC9 and H1975 cell lines[2].
Combination GMP with Osimertinib (50 nM; 12 d) and Luminespib significantly reduces the colony-forming ability of PC9, H1975, PC9-OR2 and PC9-OR4 non-small cell lung cancer cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human lung adenocarcinoma PC9, H1975, PC9-OR2, PC9-OR4 cell lines
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Concentration:500 nM, 1000 nM, 2000 nM, 2500 nM (in combination with ganetespib or luminespib)
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Incubation Time:72 h
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Result:Potentiated cell viability reduction in osimertinib-resistant PC9-OR2 and PC9-OR4 cell lines when combined with ganetespib or luminespib.
Reduced viability in both resistant lines when combined with luminespib.
Reduced viability in PC9-OR4 when combined with ganetespib.
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Cell Line:human lung adenocarcinoma PC9-OR2, PC9-OR4 osimertinib-resistant cell lines
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Concentration:50 nM (in combination with luminespib at 40, 60, 100 nM)
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Incubation Time:24 h
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Result:Increased phosphorylation of Stat3, AKT, and Src in both PC9-OR2 and PC9-OR4 when used alone.
Increased phosphorylation of YAP in PC9-OR2 when used alone.
Reversed osimertinib-induced protein phosphorylation when combined with luminespib.
Caused downregulation of YAP and AKT expression in PC9-OR4, Bcl2 expression in PC9-OR2, and Bmi1 expression in PC9-OR4 when combined with luminespib.
Caused downregulation of p14 in PC9-OR2 and p16 in PC9-OR4 when combined with luminespib.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (4- to 6-week-old female; intracranial orthotopic xenograft model of radioresistant glioblastoma)[1]
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Dosage:60 μl per 10 g body weight
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Administration:i.v.; every 48 h
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Result:Reduced tumor flux values significantly lower than control, saline + IR, free osimertinib/bortezomib + IR, iRGD-LP + IR, and Non-OB-LP + IR groups by day 15.
Extended median survival to 53.5 days, which was significantly longer than the 39.5 days observed in the saline + IR group (p < 0.0001) and the 48 days observed in the Non-OB-LP + IR group (p < 0.01).
Suppressed phosphorylated EGFR, phosphorylated ATM, and phosphorylated DNA-PKcs in tumor tissues harvested 2 h post-irradiation compared to other treatment groups.
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Animal Model:BALB/cAJcl-nu/nu nude mice (7-week-old male; intracranial stereotactic implantation of 1×104 patient-derived GS-Y03 glioma stem cells)[3]
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Dosage:5 mg/kg
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Administration:p.o.; 5 times a week
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Result:Improved survival compared to control mice, though survival was significantly shorter than in mice treated with the combination of osimertinib and brexpiprazole.
Did not cause notable adverse effects or reduce mouse body weight.
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Animal Model:BALB/c A-nu (6-week-old female)[4]
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Dosage:20 mg/L
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Administration:p.o.; continuous via drinking water; 4 weeks
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Result:Induced significant tumor shrinkage compared to vehicle control, with final mean tumor volume lower than control and chloroquine-only groups.
Increased Beclin-1 phosphorylation and slightly decreased ALDH1A1 and SOX2 protein expression in tumor tissue.
Caused no overt weight loss during the 4-week period.
Combination with chloroquine resulted in significantly greater tumor shrinkage than osimertinib alone (P < 0.05).
化学情報
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CAS 番号 1421373-65-0
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分子量 499.61
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分子式 C28H33N7O2
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SMILES
C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
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別名
AZD-9291 (GMP); Mereletinib (GMP)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Xie C, et al. GSCs differentiation model-informed nanotherapy: dual-functional brain-targeting liposomes with iRGD modification for co-delivery of osimertinib and bortezomib to combat radioresistant glioblastoma. Cell death & disease. 2025 Oct 21;16(1):738. [Content Brief]
[2]. Codony-Servat J, et al. Hsp90 inhibitors enhance the antitumoral effect of osimertinib in parental and osimertinib-resistant non-small cell lung cancer cell lines. Translational lung cancer research. 2019 Aug;8(4):340-351. [Content Brief]
[3]. Suzuki S, et al. Brexpiprazole, a Serotonin-Dopamine Activity Modulator, Can Sensitize Glioma Stem Cells to Osimertinib, a Third-Generation EGFR-TKI, via Survivin Reduction. Cancers. 2019 Jul 05;11(7):947. [Content Brief]
[4]. Li L, et al. Protective autophagy decreases osimertinib cytotoxicity through regulation of stem cell-like properties in lung cancer. Cancer letters. 2019 Jun 28;452:191-202. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Osimertinib (GMP) 関連分類
HY-15772G 関連分類
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