Erdafitinib (Synonyms: JNJ-42756493)

Name: Erdafitinib
Brand: MedChemExpress
SKU: HY-18708
Rating: 5.0 (23 reviews)

Cat. No.: HY-18708 Purity: 99.66%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

For research use only. We do not sell to patients.

Erdafitinib Chemical Structure

CAS No. : 1346242-81-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Erdafitinib:

Erdafitinib (Standard) Get quote

23 Publications Citing Use of MCE Erdafitinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

View All Isoforms

FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

IC₅₀ & Target^[1]

FGFR1

1.2 nM (IC₅₀)

FGFR2

2.5 nM (IC₅₀)

FGFR3

3.0 nM (IC₅₀)

FGFR4

5.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.02 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
AN3-CA	GI₅₀	0.048 μM Compound: 2	Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	> 5 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	> 5 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	0.005 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	0.761 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	4.011 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
HCT-116	IC₅₀	4.24 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
J82	GI₅₀	3.796 μM Compound: 2	Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
Jurkat	IC₅₀	6.81 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
K562	IC₅₀	3.02 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
KATO III stomach cancer cell line	IC₅₀	0.004 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
KMS-11	GI₅₀	0.39 μM Compound: 2	Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
Sf21	IC₅₀	3 nM Compound: JNJ-42756493	Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f	[PMID: 32278710]
Sf21	IC₅₀	36.8 nM Compound: JNJ-42756493	Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a	[PMID: 32278710]
Sf9	IC₅₀	0.003 μM Compound: 5	Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA	10.1039/C9MD90044F
SNU-16	IC₅₀	0.0007 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]

In Vitro

Erdafitinib (JNJ-42756493) 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. Erdafitinib binds FGFR1, 3, 4, and 2 with K_d values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The K_d value for VEGFR2 is higher at 6.6 nM. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC₅₀ values of 22.1, 13.2, and 25nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

446.54

Formula

C₂₅H₃₀N₆O₂

CAS No.

1346242-81-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (139.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.33 mg/mL (5.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.33 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (23.3 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (253 KB) HNMR (227 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. Perera TP, et al. Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Mol Cancer Ther. 2017 Mar 24. pii: molcanther.0589.2016. [Content Brief]

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 30 mg/kg Erdafitinib. 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	[1]. Perera TP, et al. Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Mol Cancer Ther. 2017 Mar 24. pii: molcanther.0589.2016. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2394 mL	11.1972 mL	22.3944 mL	55.9860 mL
	5 mM	0.4479 mL	2.2394 mL	4.4789 mL	11.1972 mL
	10 mM	0.2239 mL	1.1197 mL	2.2394 mL	5.5986 mL
	15 mM	0.1493 mL	0.7465 mL	1.4930 mL	3.7324 mL
	20 mM	0.1120 mL	0.5599 mL	1.1197 mL	2.7993 mL
	25 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2394 mL
	30 mM	0.0746 mL	0.3732 mL	0.7465 mL	1.8662 mL
	40 mM	0.0560 mL	0.2799 mL	0.5599 mL	1.3997 mL
	50 mM	0.0448 mL	0.2239 mL	0.4479 mL	1.1197 mL
	60 mM	0.0373 mL	0.1866 mL	0.3732 mL	0.9331 mL
	80 mM	0.0280 mL	0.1400 mL	0.2799 mL	0.6998 mL
	100 mM	0.0224 mL	0.1120 mL	0.2239 mL	0.5599 mL

Erdafitinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Erdafitinib1346242-81-6JNJ-42756493JNJ42756493JNJ 42756493FGFRApoptosisFibroblast growth factor receptorInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Erdafitinib (Synonyms: JNJ-42756493)

Customer Review

Other Forms of Erdafitinib:

Erdafitinib Related Antibodies

23 Publications Citing Use of MCE Erdafitinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Erdafitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Erdafitinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report