计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BI-1622 is an orally active, potent and highly selective HER2 ( ERBB2 ) inhibitor, with an IC 50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR . BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile
In Vitro
BI-1622 (0-5 µM, 72 h or 96 h) inhibits the proliferation of HER2-dependent cell lines. BI-1622 induces a dose-dependent decrease in pHER2 and pERK levels in NCI-H2170 HER2YVMA and PC-9 HER2YVMA cells with an accompanying decrease in DUSP6 messenger RNA levels. BI-1622 displays good permeability and no PgP-mediated efflux liability. BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Ba/F3 cells Concentration: 0-5 µM Incubation Time: 72 h or 96 h Result: Potently inhibited the proliferation of cancer cell lines dependent on amplified HER2 or an NRG-1 fusion. Inhibited different HER2 oncogenic variants and HER2WT with IC 50 values below 50 nM in tumor cell lines, while sparing EGFRWT-driven cells.
In Vivo
BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability . BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells) Dosage: 10, 30 and 100 mg/kg Administration: orally, twice daily Result: In the NCI-H2170 HER2YVMA mechanistic model, 100 mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100 mg/kg twice daily) resulted in tumor regressions. Animal Model: NMRI Foxn1nu mice (n=3 per group) Dosage: 1 mg/kg (IV); 10 and 100 mg/kg (Orally) Administration: IV, Orally; once (Pharmacokinetic Analysis) Result: Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.
Form:Solid
IC50& Target:HER2 7 nM (IC 50 ) ErbB4 EGFR CDK11B JAK3
规格
英文名称
BI-1622
生化机理
BI-1622 是一种口服活性、强效、高选择性的 HER2（ERBB2）抑制剂，IC 50 为 7 nM。BI-1622 对表皮生长因子受体的选择性超过 25 倍。在异种移植小鼠肿瘤模型中，BI-1622 表现出很高的体内抗肿瘤疗效。
储存条件
避光,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
分子量
508.53
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (196.65 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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