Erdafitinib

Manufactured by Selleck Chemicals

Sourced in United States

Erdafitinib is a laboratory reagent for research purposes. It is a small-molecule inhibitor that targets various receptor tyrosine kinases. The core function of Erdafitinib is to selectively inhibit the enzymatic activity of these receptors.

Automatically generated - may contain errors

Lab products found in correlation

19 protocols using erdafitinib

Systematic Screening of FGFR Inhibitor Efficacy

Check if the same lab product or an alternative is used in the 5 most similar protocols

3T3 cells expressing each FGFR variant were cultured in DMEM-F12 medium with 1.5% FBS for 2 weeks. The remaining 3T3 cells were mixed and treated with the indicated concentrations (0.1 nM–10 µM) of inhibitors for 5 days. The inhibitors were one multikinase FGFR inhibitor (dovitinib), five FGFR1/2/3 inhibitors (AZD4547, infigratinib, E7090, futibatinib, and pemigatinib), one pan-FGFR inhibitor (erdafitinib), and one FGFR4 inhibitor (H3B-6527). The experiment was conducted in triplicate. We calculated the number of each bar code using the MANO method. Considering the different doubling times of the transduced cells, dimethyl sulfoxide (DMSO)-treated cell mixtures were used as the reference control for scaling the bar code count of each clone. The relative growth inhibition of each cell clone was calculated as the ratio of the average read number across triplicates to that of the DMSO control. All inhibitors used in the assay, except E7090 (provided from Eisai Co., Ltd., Tokyo, Japan), were commercially purchased: dovitinib, AZD4547, infigratinib, pemigatinib (all from MedChem Express, Monmouth Junction, NJ, USA), futibatinib (Cayman Chemical, Ann Arbor, MI, USA), and erdafitinib and H3B-6527 (both from Selleckchem, Houston, TX, USA).

Nakamura I.T., Kohsaka S., Ikegami M., Ikeuchi H., Ueno T., Li K., Beyett T.S., Koyama T., Shimizu T., Yamamoto N., Takahashi F., Takahashi K., Eck M.J, & Mano H. (2021). Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer. NPJ Precision Oncology, 5, 66.

+ Open protocol

+ Expand

Cell Viability Quantification by Luminescence

Check if the same lab product or an alternative is used in the 5 most similar protocols

To determine cell viability, cells were seeded in 96 well plates at a density of 4 × 10³ cells per well. After a recovery time of 24 h, the cells were exposed to diverse compounds at different drug concentrations in triplicates. The small molecule inhibitors ponatinib, nintedanib, AZD-4547, dovitinib, erdafitinib, avapritinib, and dasatinib were purchased from Selleck Chemicals (Houston, TX, USA). Upon 72 h incubation, cell survival was determined with the commercially available CellTiter-Glo^® Luminescent Cell Viability Assay (Promega, Madison, WI, USA) according to manufacturer’s instructions and luminescence signals were measured with the Tecan infinite 200Pro (Zurich, Switzerland). Dose–response curves were generated and anti-cancer activity was expressed as IC₅₀ values calculated by GraphPad Prism 8.0.1 (GraphPad Software, La Jolla, CA, USA) using point-to-point function.

Lötsch D., Kirchhofer D., Englinger B., Jiang L., Okonechnikov K., Senfter D., Laemmerer A., Gabler L., Pirker C., Donson A.M., Bannauer P., Korbel P., Jaunecker C.N., Hübner J.M., Mayr L., Madlener S., Schmook M.T., Ricken G., Maaß K., Grusch M., Holzmann K., Grasl-Kraupp B., Spiegl-Kreinecker S., Hsu J., Dorfer C., Rössler K., Azizi A.A., Foreman N.K., Peyrl A., Haberler C., Czech T., Slavc I., Filbin M.G., Pajtler K.W., Kool M., Berger W, & Gojo J. (2021). Targeting fibroblast growth factor receptors to combat aggressive ependymoma. Acta Neuropathologica, 142(2), 339-360.

+ Open protocol

+ Expand

Immune Cell Profiling and Modulation

Check if the same lab product or an alternative is used in the 5 most similar protocols

Immune cells from mice were stained with PerCP-conjugated anti-CD4 (GK1.5, BioLegend) mAbs, APC/Cy7-conjugated anti-CD8a (53–6.7) mAbs, and the isotype monoclonal mAb. FITC-conjugated anti-I-A/I-E mAbs (M5/114.15.2, BioLegend) was used for negative gating. After pretreatment with 3 μM FGFR1-TKIs (PD173074; AZD4547; Erdafitinib, Selleck Chemicals), 3 μM mitogen-activated protein kinase (MAPK) inhibitor (MEK inhibitor U0126, Promega), MAPK siRNA (SignalSilence® p44/42 MAPK Erk1/2 siRNA, Cell Signaling Technology), 3 μM STAT3 inhibitor (S3I-201, Selleck Chemicals), or 3 µM PI3K inhibitor (BYL719, Selleck Chemicals) for 48 hr, HLA class I and HLA-DR expression on tumor cell lines was assessed via flow cytometry using anti-HLA class I antibodies (Abs) conjugated with fluorescein isothiocyanate (G46-2, BD Pharmingen) and anti-HLA-DR Abs conjugated with phycoerythrin (TU36, BD Pharmingen). HNSCC cell lines were treated with or without 50 U/ml IFN-γ for 48 hr before the assay. IgG1 (MOPC-21, BioLegend) and IgG2a (MOPC-173; BioLegend) were used as isotype controls. Intracellular IFN-γ staining were performed using Perm/Wash^TM (BD Pharmingen), Cytofix/Cytoperm^TM (BD Pharmingen), APC-conjugated anti-IFN-γ mAbs (4S.B3, BioLegend), and FITC-conjugated anti-granzyme B mAbs (GB11, BioLegend). Samples were analyzed using the CytoFLEX LX flow cytometer and CytExpert (Beckman Coulter).

Kono M., Komatsuda H., Yamaki H., Kumai T., Hayashi R., Wakisaka R., Nagato T., Ohkuri T., Kosaka A., Ohara K., Kishibe K., Takahara M., Katada A., Hayashi T., Kobayashi H, & Harabuchi Y. (2022). Immunomodulation via FGFR inhibition augments FGFR1 targeting T-cell based antitumor immunotherapy for head and neck squamous cell carcinoma. Oncoimmunology, 11(1), 2021619.

+ Open protocol

+ Expand

Cell Viability Assay Protocol

Check if the same lab product or an alternative is used in the 5 most similar protocols

Cell viability was measured using the CellTitre-Glo (CTG) luminescent cell viability assay (Promega, Madison, WI, USA). Cells were seeded in white 96 well flat bottom plates at a density of 1500–5000 cells per well, then treated the following day with drug for 72 h. Luminescence was measured using a SpectraMax L Microplate Reader (Molecular Devices, Sunnyvale, CA, USA) and compared to DMSO treated cells. BGJ398, erdafitinib, TAS-120, Trametinib and AZD8931 were all purchased from Selleck Chemicals and dissolved in DMSO.

Weickhardt A.J., Lau D.K., Hodgson-Garms M., Lavis A., Jenkins L.J., Vukelic N., Ioannidis P., Luk I.Y, & Mariadason J.M. (2022). Dual targeting of FGFR3 and ERBB3 enhances the efficacy of FGFR inhibitors in FGFR3 fusion-driven bladder cancer. BMC Cancer, 22, 478.

+ Open protocol

+ Expand

Inhibitor-based Xenopus Embryo Assay

Check if the same lab product or an alternative is used in the 5 most similar protocols

FGFR inhibitors SU5402 (catalog no. S7667), AZD4547 (catalog no. S2801), Erdafitinib (catalog no. S8401), and Ly2874455 (catalog no. S7057) were purchased from Selleckchem. CHX was purchased from Cell Signaling Technology (catalog no. 2112S). These chemical inhibitors were used to treat cells and Xenopus embryos at concentrations indicated in the figure legends.

Zhang F., Zhu X., Wang P., He Q., Huang H., Zheng T., Li Y., Jia H., Xu L., Zhao H., Colozza G., Tao Q., De Robertis E.M, & Ding Y. (2021). The cytokine FAM3B/PANDER is an FGFR ligand that promotes posterior development in Xenopus. Proceedings of the National Academy of Sciences of the United States of America, 118(20), e2100342118.

+ Open protocol

+ Expand

Tyrosine Kinase Inhibitor Evaluation

Check if the same lab product or an alternative is used in the 5 most similar protocols

Erdafitinib, infigratinib, pemigatinib, futibatinib, derazantinib, AZD4547, zoligratinib and LY2874455 were purchased from Selleck Chemicals. Rogaratinib was purchased from MedChemExpress.

, & Sibbald B. (2001). Global crusade to combat measles. CMAJ: Canadian Medical Association Journal, 164(11), 1609.

+ Open protocol

+ Expand

Erdafitinib and Anti-PD-1 Combination Therapy

Check if the same lab product or an alternative is used in the 5 most similar protocols

Erdafitinib for in vitro studies was obtained from Selleck Chem (catalog S8401). For in vivo studies, anti–PD-1 and IgG2a isotype for in vivo studies were obtained from BioXcell (anti–PD-1: catalog BE0273, clone 29F.1A12 or IgG2a: catalog BE0089, clone 2A3). Anti–PD-1 or control IgG2a was administered 3 times a week (Monday, Wednesday, and Friday) via intraperitoneal injection. Erdafitinib (12.5 mg/kg) for in vivo studies was obtained from Janssen (JNJ-42756493). The in vivo vehicle consisted of 2-hydroxypropyl-β-cyclodextrin (MilliporeSigma, 332593). Both Erdafitinib and vehicle control were administered by oral gavage twice a day from Monday to Friday.

Okato A., Utsumi T., Ranieri M., Zheng X., Zhou M., Pereira L.D., Chen T., Kita Y., Wu D., Hyun H., Lee H., Gdowski A.S., Raupp J.D., Clark-Garvey S., Manocha U., Chafitz A., Sherman F., Stephens J., Rose T.L., Milowsky M.I., Wobker S.E., Serody J.S., Damrauer J.S., Wong K.K, & Kim W.Y. (2024). FGFR inhibition augments anti–PD-1 efficacy in murine FGFR3-mutant bladder cancer by abrogating immunosuppression. The Journal of Clinical Investigation, 134(2), e169241.

+ Open protocol

+ Expand

Cell Viability Assay with CCK-8

Check if the same lab product or an alternative is used in the 5 most similar protocols

Cell counting kit-8 (CCK-8) (Vazyme, A311-01/02) assay was used to estimate drug response. Briefly, 2500 cells were seeded each well of 96-well plates with 100 μl of 10% FBS 1640 medium, and treated with BGJ398 (Selleck, S2183), AZD4547 (Selleck, S2801) or Erdafitinib (Selleck, S8401) on the 2nd day. After additional days of incubation, 10 μl CCK-8 was added into each well and incubated for 2 h. Afterwards, absorbance was measured at 450 nm with microplate reader. The IC50 values were calculated with nonlinear regression analysis by using GraphPad.

Wang Y., Shi T., Wang X., Hu J., Yu L., Liu Q., Wu N., Liu B, & Wei J. (2021). FGFR2 alteration as a potential therapeutic target in poorly cohesive gastric carcinoma. Journal of Translational Medicine, 19, 401.

+ Open protocol

+ Expand

Comprehensive Oncology Protein Analysis

Check if the same lab product or an alternative is used in the 5 most similar protocols

Saracatinib (AZD0530) and vistusertib (AZD2014) were provided by AstraZeneca. Crizotinib (S1068), alectinib (S2762), brigatinib (S8229), dasatinib (S1021), erdafitinib (S8401), debio-1347 (S7665), lorlatinib (S7536) and entrectinib (S7998) were purchased from Selleck Chemicals.
For Western Blot assays the antibodies used were: pALK Y1282/1283 (9687S), pALK Y1604 (3341S), ALK (#3333S), pAKT (#4060S), AKT (#4961S), pERK (9101S), ERK (9102S), pS6 (4858S), S6 (2217S), cleaved Parp (9541S), BIM (2933S), Merlin (1288S), pPaxillin (2541S), Paxillin (2542S), Snail (3879S) and Vimentin (5741S) purchased from Cell Signaling Technology.
For IHC assays the antibodies used were ALK (#6679072001), E-Cadh (#790-4497) and CD31 (#760-4378) purchased from Ventana; N-Cadh (#M3613), Ki-67 (#M7240), beta catenin (#M3539), podoplanin (#M3619) and CD68 (#M0814) purchased from DAKO; Vimentin (#790-2917) purchased from Roche; pSRC (#6943S) and pMAPK (#4376) purchased from Cell Signaling Technology; Glut1 (#RP128-05) purchased from Clinisciences; CA-IX (#NB100-417SS) purchased from NovusBio, NF2/Merlin purchased from Sigma-aldrich (#HPA003097) and CD47 (#M5792) purchased from Spring.

Recondo G., Mezquita L., Facchinetti F., Planchard D., Gazzah A., Bigot L., Rizvi A.Z., Frias R.L., Thiery J.P., Scoazec J.Y., Sourisseau T., Howarth K., Deas O., Samofalova D., Galissant J., Tesson P., Braye F., Naltet C., Lavaud P., Mahjoubi L., Abou Lovergne A., Vassal G., Bahleda R., Hollebecque A., Nicotra C., Ngo-Camus M., Michiels S., Lacroix L., Richon C., Auger N., De Baere T., Tselikas L., Solary E., Angevin E., Eggermont A., André F., Massard C., Olaussen K.A., Soria J.C., Besse B, & Friboulet L. (2019). Diverse resistance mechanisms to the third-generation ALK inhibitor lorlatinib in ALK-rearranged lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research, 26(1), 242-255.

+ Open protocol

+ Expand

Quantifying 4T07 Spheroid Growth Inhibition

Check if the same lab product or an alternative is used in the 5 most similar protocols

4T07 cells (1×10⁴) were plated into a non-adherent round bottom spheroid plate (4520; Corning) in 200 μl of DMEM containing 10% FBS and Pen/strep as described above in the cell lines section. After 48 hours, these spheroids were transferred via a 200 μl micropipette to a 50μl bed of Cultrex basement membrane matrix (3432-001-01; Trevigen) in a white-walled 96-well dish with 150 ml of full growth media containing 10% Cultrex. This was done in the presence or absence of 50 or 100 nM FIIN4 or 100 nM AZD4547 (Sellekchem), or 100 nM Erdafitinib (Selleckchem). Spheroid growth was tracked by bioluminescence as determined by adding 30 ng of D-luciferin dissolved in 2 μl of PBS immediately following transfer of the spheroids to the Cultrex and 6 days thereafter. Luminescence was read on a Glo-max Discover (Promega) plate reader.

Akhand S.S., Liu Z., Purdy S.C., Abdullah A., Lin H., Cresswell G.M., Ratliff T.L, & Wendt M. (2020). Pharmacological inhibition of FGFR modulates the metastatic immune microenvironment and promotes response to immune checkpoint blockade. Cancer immunology research, 8(12), 1542-1553.

+ Open protocol

+ Expand

About PubCompare

Our mission is to provide scientists with the largest repository of trustworthy protocols and intelligent analytical tools, thereby offering them extensive information to design robust protocols aimed at minimizing the risk of failures.

We believe that the most crucial aspect is to grant scientists access to a wide range of reliable sources and new useful tools that surpass human capabilities.

However, we trust in allowing scientists to determine how to construct their own protocols based on this information, as they are the experts in their field.

Ready to get started?

Revolutionizing how scientists
search and build protocols!