| 产品描述： | EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers |
| 靶点： |
EGFR (WT):7.92 nM (IC50);EGFR (C797S/T790M/L858R):0.218 nM (IC50) |
| 体外研究： |
EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively. EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM. EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM. EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM. Cell Proliferation Assay Cell Line: A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) suspension cells Concentration: 1 mM; 10 μM-0.508 nM Incubation Time: 3 days Result: Inhibited proliferation in cells. |
| 体内研究： |
EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o.; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model. EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model. Animal Model: Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g) Dosage: 5, 15, 45 mg/kg Administration: Oral administration, daily, for 13 days Result: Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice. Animal Model: Subcutaneous xenograft PC-9 (Δ19del) model Dosage: 0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg Administration: Oral administration, once a day, 3 weeks Result: Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy. |
| 参考文献： |
1. Ling WY, et, al. Prostaglandin E2 suppresses bacterial killing in alveolar macrophages by inhibiting NADPH oxidase. WO2019015655A1. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.44 ml |
7.198 ml |
14.397 ml |
| 5 mM |
0.288 ml |
1.44 ml |
2.879 ml |
| 10 mM |
0.144 ml |
0.72 ml |
1.44 ml |
| 50 mM |
0.029 ml |
0.144 ml |
0.288 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京