1. Protein Tyrosine Kinase/RTK
  2. FGFR

Erdafitinib (Synonyms: JNJ-42756493)

Cat. No.: HY-18708 Purity: 99.54%
Data Sheet SDS Handling Instructions

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1-4 with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively.

For research use only. We do not sell to patients.
Erdafitinib Chemical Structure

Erdafitinib Chemical Structure

CAS No. : 1346242-81-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $120 In-stock
50 mg $350 In-stock
100 mg $600 In-stock
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500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1-4 with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively.

IC50 & Target

IC50: 1.2 nM (FGFR1), 2.5 nM (FGFR2), 3.0 nM (FGFR3)and 5.7 nM (FGFR4)[1]

In Vitro

Erdafitinib inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8 nM. JNJ-42756493 binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd value for VEGFR2 is higher at 6.6 nM. JNJ-42756493 inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively[1].

In Vivo

In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT03066687 Janssen Research & Development, LLC|Celerion Healthy March 14, 2017 Phase 1
NCT03135106 Janssen Research & Development, LLC Healthy April 14, 2017 Phase 1
NCT02699606 Janssen Research & Development, LLC Neoplasm July 8, 2016 Phase 2
NCT02421185 Janssen Research & Development, LLC Carcinoma, Hepatocellular May 25, 2015 Phase 1
NCT02692677 Janssen Research & Development, LLC Healthy March 2016 Phase 1
NCT02231489 Janssen Research & Development, LLC Healthy September 2014 Phase 1
NCT03210714 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|FGFR1 Gene Mutation|FGFR2 Gene Mutation|FGFR3 Gene Mutation|FGFR4 Gene Mutation|Histiocytosis|Low Grade Glioma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumo November 30, 2017 Phase 2
NCT01962532 Janssen Research & Development, LLC Neoplasms|Lymphoma|Adenocarcinoma|Esophagogastric Junction August 2013 Phase 1
NCT02365597 Janssen Research & Development, LLC Urothelial Cancer April 22, 2015 Phase 2
NCT01703481 Janssen Research & Development, LLC Tumor or Lymphoma June 15, 2012 Phase 1
NCT02218073 Janssen Research & Development, LLC Healthy October 2014 Phase 1
NCT02466815 Janssen Research & Development, LLC Healthy June 2015 Phase 1
NCT02952573 University Health Network, Toronto Multiple Myeloma|Relapsed/Refractory January 2017 Phase 2
NCT03155620 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Childhood Langerhans Cell Histiocytosis|Histiocytic Sarcoma|Juvenile Xanthogranuloma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell July 24, 2017 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.2394 mL 11.1972 mL 22.3944 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 mL
Cell Assay
[1]

Erdafitinib is dissolved in DMSO. KATO III, RT-112, A-204, RT-4, DMS-114, A-427 and MDA-MB-453 cells are treated with erdafitinib (from 10 μM to 0.01 nM in 2% DMSO, final concentration). Following 4-day incubation, cell viability is determined using MTT reagent. The optical density is determined at 540 nm[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mouse: Mice bearing SNU-16 human gastric carcinoma (FGFR2 amplified) xenograft tumors are dosed orally with 0, 3, 10 or 30mg/kg JNJ-42756493. Tumor tissue and mouse plasma (3 mice per time point) are harvested at 0.5, 1, 3, 7, 16 and 24h post-dosing[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

446.54

Formula

C₂₅H₃₀N₆O₂

CAS No.

1346242-81-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Erdafitinib
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