上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
EGFR-IN-47
EGFR-IN-47 是一种有效的且具有口服活性的 EGFRL858R/T790M/C797S 抑制剂，其 IC50 值为 0.01 µM。EGFR-IN-47 诱导细胞周期停滞和细胞凋亡 (apoptosis)。EGFR-IN-47 具有 NSCLC 的研究潜力。
EGFR-IN-47 Chemical Structure
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
EGFR-IN-47 is a potent and orally active EGFRL858R/T790M/C797S inhibitor with an IC50 of 0.01 µM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC[1].
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| IC50 & Target[1] |
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EGFRL858R/T790M/C797S
0.07 μM (IC50)
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体外研究
(In Vitro) |
EGFR-IN-47 (compound 14aj) (72 h) shows anti-proliferative effects with IC50s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 µM; 24 h) induces cell cycle attest at the G0/G1-phase[1].
EGFR-IN-47 (0.01, 0.05, 0.25 µM) induces cell deathvia apoptosis in a concentration-dependent manner[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 µM) inhibits phosphorylation of the EGFR downstream mediators[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay[1]
| Cell Line: |
PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells |
| Concentration: |
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| Incubation Time: |
72 h |
| Result: |
Showed anti-proliferative effects with IC50s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively. |
Cell Cycle Analysis[1]
| Cell Line: |
PC-9 EGFRL858R/T790M/C797S cells |
| Concentration: |
0.01, 0.05, 0.25, 1 µM |
| Incubation Time: |
24 h |
| Result: |
Cells were arrest at the G0/G1-phase. |
Apoptosis Analysis[1]
| Cell Line: |
PC-9 EGFRL858R/T790M/C797S cells |
| Concentration: |
0.01, 0.05, 0.25 µM |
| Incubation Time: |
24 h |
| Result: |
Induced cell deathvia apoptosis in a concentration-dependent manner. |
Western Blot Analysis[1]
| Cell Line: |
PC-9 EGFRL858R/T790M/C797S cells |
| Concentration: |
0.01, 0.05, 0.25, 1 µM |
| Incubation Time: |
|
| Result: |
Inhibited phosphorylation of the EGFR downstream mediators. |
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体内研究
(In Vivo) |
EGFR-IN-47 (10, 20, 40 mg/kg; i.g.) shows anti-tumor effect with low toxicity[1].
EGFR-IN-47 (20 mg/kg for i.v.; 20 mg/kg for p.o.) shows an ideal oral bioavailability of 66.05%[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley rats[1].
| parameter |
iv (20 mg/kg) |
po (20 mg/kg) |
| AUC0-∞ (mg/Lh) |
15.889 |
10.494 |
| Cmax (mg/L) |
6.845 |
0.77 |
| Tmax (h) |
0.083 |
6 |
| F (%) |
|
66.05 |
| MRT0-∞ (h) |
16.439 |
16.791 |
| Vss (L/kg) |
16.015 |
28.101 |
| CL (L/h/kg) |
1.272 |
2.151 |
| t(1/2) (h) |
8.922 |
11.154 |
Male Sprague-Dawley rats; 20 mg/kg for i.v.; 20 mg/kg for p.o.[1]
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
6-8 weeks, BALB/c nude mice (PC-9 EGFRL858R/T790M/C797S cells )[1] |
| Dosage: |
10, 20, 40 mg/kg (dissolved in 25% (v/v) PEG400 plus 5% DMSO) |
| Administration: |
I.g. |
| Result: |
Showed anti-tumor effect with low toxicity. |
| Animal Model: |
Male Sprague-Dawley rats[1] |
| Dosage: |
20 mg/kg |
| Administration: |
I.v.; p.o. |
| Result: |
Showed an ideal oral bioavailability of 66.05%. |
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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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