- ￥490 - 1490
- Solarbio
- 北京
- IE0900
- 2025年07月23日
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
EAI-045
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1942114-09-1
- 规格：
50mg/25mg/5mg/10mg
| 规格： | 50mg | 产品价格： | ￥1490.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥1070.0 |
| 规格： | 5mg | 产品价格： | ￥490.0 |
| 规格： | 10mg | 产品价格： | ￥710.0 |
| 基本信息 | |
| CAS | No.1942114-09-1 |
| 英文名称 | EAI-045 |
| 分子式 | C19H14FN3O3S |
| 分子量 | 383.4 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to brown Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD30187871 |
| SMILES | O=C(C(C1=C(O)C=CC(F)=C1)N2C(C(C=CC=C3)=C3C2)=O)NC4=NC=CS4 |
| InChIKey | YTUFHOKUFOQRDF-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H14FN3O3S/c20-12-5-6-15(24)14(9-12)16(17(25)22-19-21-7-8-27-19)23-10-11-3-1-2-4-13(11)18(23)26/h1-9,16,24H,10H2,(H,21,22,25) |
| PubChem CID | 121231412 |
| 靶点 | EGFR |
| 通路 | Angiogenesis;Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
| 背景说明 | EAI-045是突变体EGFR变构抑制剂。 |
| 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.[1-2] |
| 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 数据来源文献 | [1]. Jia Y， et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32. [2]. Wang S， et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54. |
| 单位 | 瓶 |
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
技术资料暂无技术资料 索取技术资料
IE0900 EAI-045 血管生成 索莱宝
￥490 - 1490
