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。
Cas No.:1443530-05-9
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells |
Preparation Method | MDA-MB-231 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin at 37℃ in the presence of 5% CO2. 6×103 cells per well were seeded in a 96-well plate for 24h, and were treated with different concentrations of Rogaratinib (0.001, 0.01, 0.1, 1, and 10µM). After a 72-hour incubation with Rogaratinib, cell viability was measured. |
Reaction Conditions | 0.001, 0.01, 0.1, 1, and 10µM; 72h |
Applications | Rogaratinib treatment significantly reduced the cell viability of MDA-MB-231 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/cJ mice |
Preparation Method | Female BALB/cJ mice (18-21g; 5-6 weeks) were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility. Mice were injected subcutaneously (s.c.) in the left inguinal region with 1×106 syngeneic C51 colon cancer cells as a suspension in 0.1ml 50% matrigel/50% medium. The mice were randomized (n =10/group) (average tumor volume 100mm3) and treated orally (p.o.) for 13 days with vehicle or Rogaratinib (75mg/kg/day). Measure the tumor volume and weight every two days. |
Dosage form | 75mg/kg/day for 13 days; p.o. |
Applications | Rogaratinib treatment inhibited the tumor growth in mice with C51 cell xenografts. |
References: | |
| Cas No. | 1443530-05-9 | SDF | |
| 别名 | 罗加替尼,BAY1163877 | ||
| Canonical SMILES | O=C1NCCN(CC2=C(COC)C(C3=CC4=CC(C)=CC(OC)=C4S3)=C5C(N)=NC=NN52)C1 | ||
| 分子式 | C23H26N6O3S | 分子量 | 466.56 |
| 溶解度 | DMSO : 6 mg/mL (12.86 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1433 mL | 10.7167 mL | 21.4335 mL |
| 5 mM | 428.7 μL | 2.1433 mL | 4.2867 mL |
| 10 mM | 214.3 μL | 1.0717 mL | 2.1433 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00% Appearance: A solid
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