Erdafitinib是一种口服的选择性酪氨酸激酶抑制剂，抑制FGFR家族（FGFR1：IC50 = 1.2nM；FGFR2：IC50 = 2.5nM；FGFR3：IC50 = 3.0nM；FGFR4：IC50 = 5.7nM）。
Cas No.:1346242-81-6
Sample solution is provided at 25 µL, 10mM.
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Erdafitinib is an orally available, selective tyrosine kinase inhibitor of the entire FGFR family (FGFR1: IC50 = 1.2nM; FGFR2: IC50 = 2.5nM; FGFR3: IC50 = 3.0nM; FGFR4: IC50 = 5.7nM) [1]. Erdafitinib inhibits the proliferation and survival of cells with abnormal FGFR genes (such as FGFR3 or FGFR2 variants) by blocking phosphorylation and downstream signaling pathways, thereby inducing apoptosis [2-3]. Erdafitinib is primarily used to treat advanced or metastatic urothelial carcinoma harboring FGFR2/3 genetic abnormalities [4].
In HEK293 ABCB1 overexpressing cells, Erdafitinib (0.06-0.6μM; 2 h) enhances the sensitivity of cells to chemotherapeutic drugs [5]. In BV2 microglial cells, Erdafitinib (0.1-20μM; 24h) pretreatment decreases LPS-mediated proinflammatory cytokine expression through NLRP3 [6]. In MDA-MB-231 cells, Erdafitinib (0-100μM; 24h) inhibited the growth of cells in a dose-dependent manner [7].
In A549 cells xenograft tumor mouse model, Erdafitinib (10mg/kg; ip; 21d) suppresses tumor growth, accompanied by decreased CDK2 expression [8]. In SRM KO MGH-U3 cells xenograft tumor mouse model, combination of SRM deletion and Erdafitinib (5mg/kg, 15mg/kg; po; 4 weeks) targeted therapy elicited a complete inhibition of tumor growth [9].
References:
[1]. Perera T P S, Jovcheva E, Mevellec L, et al. Discovery and pharmacological characterization of JNJ-42756493 (Erdafitinib), a functionally selective small-molecule FGFR family inhibitor[J]. Molecular cancer therapeutics, 2017, 16(6): 1010-1020.
[2]. Haura E B, Hicks J K, Boyle T A. Erdafitinib overcomes FGFR3-TACC3–mediated resistance to osimertinib[J]. Journal of Thoracic Oncology, 2020, 15(9): e154-e156.
[3]. Kaur J, Singh A, Shah M, et al. Erdafitinib for tumors with FGFR3 mutation: A promising targeted therapy[J]. Cancer Research, Statistics, and Treatment, 2023, 6(2): 288-295.
[4]. Guercio B J, Sarfaty M, Teo M Y, et al. Clinical and genomic landscape of FGFR3-altered urothelial carcinoma and treatment outcomes with erdafitinib: a real-world experience[J]. Clinical Cancer Research, 2023, 29(22): 4586-4595.
[5]. Feng W, Zhang M, Wu Z X, et al. Erdafitinib antagonizes ABCB1-mediated multidrug resistance in cancer cells[J]. Frontiers in oncology, 2020, 10: 955.
[6]. Lee H, Kim S H, Jung T M, et al. Erdafitinib diminishes LPS-mediated neuroinflammatory responses through NLRP3 in wild-type mice[J]. Frontiers in Pharmacology, 2025, 16: 1572604.
[7]. Luo Q, Zhang L, Hao Y, et al. Erdafitinib inhibits the tumorigenicity of MDA-MB-231 triple-negative breast cancer cells by inducing TRIM25/ubiquitin-dependent degradation of FGFR4[J]. Breast Cancer Research, 2025, 27(1): 128.
[8]. Meng X, Zhu X, Ji J, et al. Erdafitinib inhibits tumorigenesis of human lung adenocarcinoma A549 by inducing S-phase cell-cycle arrest as a CDK2 inhibitor[J]. Molecules, 2022, 27(19): 6733.
[9]. Yu Y, Gao X, Zhao H, et al. A Genome-Wide Synthetic Lethal Screen Identifies Spermidine Synthase as a Target to Enhance Erdafitinib Efficacy in FGFR-Mutant Bladder Cancer[J]. Cancer Research, 2025, 85(12): 2288-2301.
Erdafitinib是一种口服的选择性酪氨酸激酶抑制剂，抑制FGFR家族（FGFR1：IC50 = 1.2nM；FGFR2：IC50 = 2.5nM；FGFR3：IC50 = 3.0nM；FGFR4：IC50 = 5.7nM） [1]。Erdafitinib通过阻断FGFR基因异常（例如FGFR3或FGFR2变体）的磷酸化和下游信号通路，抑制其增殖和存活，从而诱导细胞凋亡 [2-3]。Erdafitinib主要用于治疗伴有FGFR2/3基因异常的晚期或转移性尿路上皮癌 [4]。
在HEK293 ABCB1过表达细胞中，Erdafitinib（0.06-0.6μM；2h）增强细胞对化疗药物的敏感性 [5]。在BV2小胶质细胞中，Erdafitinib（0.1-20μM；24h）预处理可通过NLRP3降低LPS介导的促炎细胞因子表达 [6]。在MDA-MB-231细胞中，Erdafitinib（0-100μM；24h）以剂量依赖性方式抑制细胞的生长 [7]。
在A549细胞异种移植瘤小鼠模型中，Erdafitinib（10mg/kg；ip；21d）可抑制肿瘤生长，并伴随CDK2表达降低 [8]。在SRM KO MGH-U3细胞异种移植肿瘤小鼠模型中，SRM缺失和Erdafitinib（5mg/kg，15mg/kg；po；4周）靶向治疗相结合，可完全抑制肿瘤生长 [9]。
| Cell experiment [1]: | |
Cell lines | HEK293 ABCB1 overexpressing cells |
Preparation Method | For reversal study, different concentrations of paclitaxel, vincristine, or cisplatin were added into the wells after cells pre-incubated with different concentrations (0.06, 0.2, or 0.6μM) of Erdafitinib for 2h. The cells were incubated for 72h. |
Reaction Conditions | 0.06-0.6μM; 2h |
Applications | Erdafitinib increased the sensitivity of chemotherapeutic drugs in HEK293 ABCB1 overexpressing cells. |
| Animal experiment [2]: | |
Animal models | A549 cells xenograft tumor mouse model |
Preparation Method | A549-Luc cells (5 × 107) were mixed with Matrigel (2:1) and injected subcutaneously into BALB/c nude mice. The mice were randomly divided into two groups (n = 3 per group): vehicle and Erdafitinib (10mg/kg), when the tumor volumes reached approximately 100mm3. Body weight and tumor volumes were measured every other day. |
Dosage form | 10mg/kg; ip; 21d |
Applications | In A549 cells xenograft tumor mouse model, Erdafitinib suppresses tumor growth suppresses tumor growth, accompanied by decreased CDK2 expression. |
References: | |
| Cas No. | 1346242-81-6 | SDF | |
| 别名 | 厄达替尼; JNJ-42756493 | ||
| Canonical SMILES | CN1N=CC(C2=NC3=CC(N(C4=CC(OC)=CC(OC)=C4)CCNC(C)C)=CC=C3N=C2)=C1 | ||
| 分子式 | C25H30N6O2 | 分子量 | 446.54 |
| 溶解度 | DMSO : ≥ 33 mg/mL (73.90 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 | 2.2394 mL | 11.1972 mL | 22.3944 mL |
| 5 mM | 447.9 μL | 2.2394 mL | 4.4789 mL |
| 10 mM | 223.9 μL | 1.1197 mL | 2.2394 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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