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。
EAI045 纯度: 98.90%
EAI045是突变体 EGFR 的第四代变构抑制剂,在10 μM ATP时抑制EGFR,EGFRL858R,EGFRT790M 和 EGFRL858R/T790M 的IC50 值分别为1.9,0.019,0.19 和 0.002 μM。
EAI045 Chemical Structure
CAS No. : 1942114-09-1
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1650 | In-stock | |
50 mg | ¥1500 | In-stock | |
100 mg | ¥2500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
EAI045 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Immunology/Inflammation Compound Library
- JAK/STAT Compound Library
- Kinase Inhibitor Library
- Protein Tyrosine Kinase Compound Library
- Anti-Cancer Compound Library
- Differentiation Inducing Compound Library
- Anti-Hepatitis C Virus Compound Library
- Anti-Lung Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Angiogenesis Related Compound Library
- Targeted Diversity Library
- Anti-Liver Cancer Compound Library
- Anti-Colorectal Cancer Compound Library
生物活性 |
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively. |
||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target |
|
||||||||||||||||
体外研究 (In Vitro) |
EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM), but not in HaCaT cells. EAI045 is an inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wild type EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 protein kinases reveals exquisite selectivity; no other kinases are inhibited by more than 20% at 1 μM EAI045[1]. EAI045 has high potency and selectivity for L858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045 decreases but does not completely abolish the EGFR autophosphorylation. In stably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045 shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderate activity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR, EAI045 does not show any activity of inhibiting EGFR phosphorylation. It confirms the selectivity of EAI045 for mutant EGFR[2]. 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. |
||||||||||||||||
体内研究 (In Vivo) |
In a genetically engineered mouse model of L858R/T790Mmutant-driven lung cancer , remarkable tumor regression is observed in L858R/T790M-mutant mice treated with the combination of EAI045 and cetuximab. No response is seen in those mice treated with EAI045 alone. The same effect is seen in both L858R/T790M/C797S- engineered Ba/F3 cells and in mice carrying the L858R/T790M/C797S tumor xenografts. These assays clearly show that EAI045 can overcome resistance from acquired T790M and C797S mutations[2]. 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. |
||||||||||||||||
分子量 |
383.40 |
||||||||||||||||
Formula |
C19H14FN3O3S |
||||||||||||||||
CAS 号 |
1942114-09-1 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (260.82 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
|
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
For the experiment studying the effect of EGF pre-treatment on EAI045 target modulation, H1975 cells are harvested and plated in 0.5% FBS/RPMI Pen/Strep. On the following day, cells are pre-treated with 0.5% FBS/RPMI media with or without 10 ng EGF/mL for 5 minutes. Compound is added and assay is carried out[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 Administration [1] |
Mice: Cetuximab is administrated at 1 mg/mouse every other day by intraperitoneal injection. The TL, TD and TLCS mice are monitored by MRI to quantify lung tumor burden before being assigned to various study treatment cohorts, which are non-blinded and not formally randomized. All treated mice had an equal initial tumor burden. MRI evaluation is repeated every 2 weeks during treatment. The animals are imaged with a rapid acquisition with relaxation enhancement sequence in the coronal and axial planes with a 1-mm slice thickness gating with respiratory rates. The tumor burden volumes are quantified[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. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务