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Erdafitinib

CAT: 0013-GTR19163793-05Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163793-05Size:10 mg
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Description
Erdafitinib (JNJ-42756493) is a highly potent and selective, small-molecule inhibitor of FGFR family with IC50s of 1.2/2.5/3/5.7 nM for FGFR1/2/3/4; shows rapid uptake into the lysosomal compartment of cells in culture, which is associated with prolonged inhibition of FGFR signaling; orally active.Blood Cancer Phase 2 Clinical (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 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. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively. (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.
CAS Number
1346242-81-6
Product Name Alternative
JNJ-42756493
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 33 mg/mL
Smiles
CC (NCCN (C1=CC (OC) =CC (OC) =C1) C2=CC=C3N=CC (C4=CN (C) N=C4) =NC3=C2) C
Molecular Formula
C25H30N6O2
Molecular Weight
446.5447
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1,2-Ethanediamine, N1- (3,5-dimethoxyphenyl) -N2- (1-methylethyl) -N1-[3- (1-methyl-1H-pyrazol-4-yl) -6-quinoxalinyl]-

Chemical Information

Erdafitinib

Erdafitinib is a Kinase Inhibitor. The mechanism of action of erdafitinib is as a Fibroblast Growth Factor Receptor Inhibitor, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A4 Inducer, and P-Glycoprotein Inhibitor, and Organic Cation Transporter 2 Inhibitor.

CAS Number1346242-81-6
PubChem CID67462786
IUPAC NameN'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine
Molecular FormulaC25H30N6O2
Molecular Weight446.5
XLogP3.2
Topological Polar Surface Area77.3
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count9
Heavy Atom Count33
Formal Charge0
Complexity583
SMILES
CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
InChI
InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
InChIKey
OLAHOMJCDNXHFI-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Erdafitinib
CAS: 1346242-81-6
CID: 67462786
Formula: C25H30N6O2
MW: 446.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight446.5
XLogP33.2
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count9
Exact Mass446.24302422
Monoisotopic Mass446.24302422
Topological Polar Surface Area77.3 Ų
Heavy Atom Count33
Formal Charge0
Complexity583
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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CatalogName
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