Pemigatinib

国际站：Pemigatinib

CAS：1513857-77-6

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性： Pemigatinib (INCB054828) 是一种具有口服活性的选择性 FGFR 抑制剂，IC₅₀ 分别为 0.4 nM、0.5 nM、1.2 nM、30 nM，用于分别为 FGFR1、FGFR2、FGFR3、FGFR4。 Pemigatinib 具有潜在的胆管癌^[1][2]。 

体外：这一假设得到体外细胞研究的证实，其中表达 FGFR2-CLIP1 融合的细胞对 Pemigatinib 敏感（INCB054828；IC₅₀ 值为 10.16 nM），而添加 N549H 突变的细胞对 Pemigatinib 具有耐药性（IC₅₀ 值为 1527.57 nM）^[3]。

参考文献：[1]. Arudra K, et al. Calcinosis cutis dermatologic toxicity associated with fibroblast growth factor receptor inhibitor for the treatment of Wilms tumor. J Cutan Pathol. 2018 Oct;45(10):786-790.[2]. Roskoski R Jr, et al. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567.[3]. Krook MA, et al. Tumor heterogeneity and acquired drug resistance in FGFR2-fusion-positive cholangiocarcinoma through rapid research autopsy. Cold Spring Harb Mol Case Stud. 2019 Aug 1;5(4).