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Erdafitinib

Cat. No. M9715
Erdafitinib Structure
Synonym:

JNJ-42756493

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 75  USD75 In stock
25mg USD 140  USD140 In stock
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Quality Control & Documentation
Biological Activity

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan FGFR inhibitor with potential antineoplastic activity. Erdafitinib (JNJ-42756493) inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

In vivo, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors.

Product Citations
Chemical Information
Molecular Weight 446.54
Formula C25H30N6O2
CAS Number 1346242-81-6
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kamaneh Montazeri, et al. Expert Rev Clin Pharmacol. Erdafitinib for the treatment of metastatic bladder cancer

[2] Timothy P S Perera, et al. Mol Cancer Ther. Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

[3] Maud Verstraete, et al. BMC Cancer. In vitro and in vivo evaluation of the radiosensitizing effect of a selective FGFR inhibitor (JNJ-42756493) for rectal cancer

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Keywords: Erdafitinib, JNJ-42756493 supplier, FGFR, inhibitors, activators


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