Rogaratinib (BAY1163877) is a potent, selective, and oral orally available fibroblast growth factor receptor (FGFR) inhibitor, with IC50 values of 12nM, 19nM, 33nM, and 120nM for FGFR-1, FGFR-3, FGFR-4, and VEGFR-2, respectively [1]. Rogaratinib reversibly blocks the ATP-binding pocket of FGFR1-4 kinase domains, thereby inhibiting the downstream signal transduction[2]. Rogaratinib has been widely used to inhibit the development of breast cancer in cell models and animal models, as well as to develop new combined therapies[3].
In vitro, Rogaratinib treatment for 72 hours significantly inhibited the viability of MCF-10A cells, MDA-MB-231 cells and MCF-7 cells, with IC50 values of 9.5μM, 0.1μM, and 1.0μM, respectively[4].
In vivo, Rogaratinib treatment via oral administration at a dose of 75mg/kg/day for 13 days significantly inhibited tumor growth in a C51 xenograft colon cancer mouse model[5].
References:
[1] Collin M P, Lobell M, Hübsch W, et al. Discovery of Rogaratinib (BAY 1163877): a pan‐FGFR inhibitor[J]. ChemMedChem, 2018, 13(5): 437-445.
[2] Dedousis D, Gadra E, Van Galen J, et al. Recent advances in succinate dehydrogenase deficient gastrointestinal stromal tumor systemic therapies[J]. Current Treatment Options in Oncology, 2025, 26(4): 227-240.
[3] Politz O, Ellinghaus P, Bender S, et al. Preclinical activity of the FGFRinhibitor BAY 1163877 alone or in combination with antihormonal therapy in breast cancer[J]. Cancer Research, 2017, 77(13_Supplement): 1079-1079.
[4] Cui Y, Zhang L, Xing J, et al. Research on mechanism of FGFR1 inhibitor BAY1163877 against proliferation of breast cancer cells[C]//IOP Conference Series: Materials Science and Engineering. IOP Publishing, 2019, 562(1): 012128.
[5] Grünewald S, Politz O, Bender S, et al. Rogaratinib: A potent and selective pan‐FGFR inhibitor with broad antitumor activity in FGFR‐overexpressing preclinical cancer models[J]. International journal of cancer, 2019, 145(5): 1346-1357.
Rogaratinib (BAY1163877)是一种强效、选择性、口服可用的成纤维细胞生长因子受体（FGFR）抑制剂，对FGFR-1、FGFR-3、FGFR-4和VEGFR-2的IC50值分别为12nM、19nM、33nM和120nM[1]。Rogaratinib可逆地阻断FGFR1-4激酶结构域的ATP结合口袋，从而抑制下游信号转导[2]。Rogaratinib已被广泛用于抑制细胞模型和动物模型中的乳腺癌发展，并用于开发新型联合疗法[3]。
在体外，Rogaratinib处理72小时显著抑制了MCF-10A细胞、MDA-MB-231细胞和MCF-7细胞的活力，IC50值分别为9.5μM、0.1μM和1.0μM[6]。
在体内，每日口服75mg/kg剂量的Rogaratinib，连续13天，显著抑制了C51异种移植结肠癌小鼠模型中的肿瘤生长[8]。