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Erdafitinib

Cat. No. M9715
Erdafitinib Structure
Synonym:

JNJ-42756493

Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 105  USD105 In stock
50mg USD 425  USD425 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 446.54
Formula C25H30N6O2
CAS Number 1346242-81-6
Purity >99%
Solubility DMSO ≥ 40 mg/mL
Storage at -20°C
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

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