1. Protein Tyrosine Kinase/RTK
  2. FGFR

Erdafitinib (Synonyms: JNJ-42756493)

Cat. No.: HY-18708 Purity: 98.77%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 350 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Protocol

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  • 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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (73.90 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
References
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]

Mice: 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

SMILES

CN1N=CC(C2=NC3=CC(N(C4=CC(OC)=CC(OC)=C4)CCNC(C)C)=CC=C3N=C2)=C1

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

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Product Name:
Erdafitinib
Cat. No.:
HY-18708
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Erdafitinib

Cat. No.: HY-18708