BI-1622|2681392-19-6|-陌孚医药/Medlife

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BI-1622

目录号: PL04314 纯度: ≥98%

CAS No. :2681392-19-6

商品编号	规格	价格	会员价
PL04314-5mg	5mg	询价	询价
PL04314-10mg	10mg	询价	询价
PL04314-25mg	25mg	询价	询价

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中文名称	BI-1622
中文别名	化合物 BI-1622
英文名称	BI-1622
英文别名	BI-1622
Cas No.	2681392-19-6
分子式	C₂₆H₂₄N₁₀O₂
分子量	508.53
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	BI-1622 是一种口服有效的和高选择性 HER2 (ERBB2) 抑制剂，IC₅₀ 为 7 nM。BI-1622对 EGFR 的选择性大于 25 倍。BI-1622 在转染 H2170 和 PC9 细胞的移植瘤小鼠模型中表现出较高的体内的抗肿瘤效果，具有良好的药物代谢和药代动力学特性。
生物活性	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 drug metabolism and pharmacokinetics profile.
性状	Solid
IC50 & Target[1][2]	HER2 7 nM (IC50) ErbB4
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献	[1]. Lamarre L, et al. Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer. 2022 Jul;3(7):821-836.

溶解度数据	In Vitro: DMSO : 100 mg/mL (196.65 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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