Erdafitinib
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MedKoo CAT#: 206440

CAS#: 1346242-81-6

Description: Erdafitinib, also known as JNJ-42756493, is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, JNJ-42756493 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumor cell proliferation and tumor cell death in FGFR-overexpressing tumor cells. FGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival.


Chemical Structure

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Erdafitinib
CAS# 1346242-81-6

Theoretical Analysis

MedKoo Cat#: 206440
Name: Erdafitinib
CAS#: 1346242-81-6
Chemical Formula: C25H30N6O2
Exact Mass: 446.24302
Molecular Weight: 446.55
Elemental Analysis: C, 67.24; H, 6.77; N, 18.82; O, 7.17

Price and Availability

Size Price Availability Quantity
25.0mg USD 90.0 Same day
50.0mg USD 150.0 Same day
100.0mg USD 250.0 Same day
200.0mg USD 450.0 Same day
500.0mg USD 950.0 Same day
1.0g USD 1750.0 Same day
2.0g USD 2950.0 Same day
5.0g USD 4650.0 Same day
10.0g USD 7950.0 2 weeks
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Synonym: JNJ-42756493; JNJ 42756493; JNJ42756493; Erdafitinib

IUPAC/Chemical Name: N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine

InChi Key: OLAHOMJCDNXHFI-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: CC(NCCN(C1=CC(OC)=CC(OC)=C1)C2=CC=C3N=CC(C4=CN(C)N=C4)=NC3=C2)C

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 446.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Montazeri K, Bellmunt J. Erdafitinib for the treatment of metastatic bladder cancer. Expert Rev Clin Pharmacol. 2019 Dec 6. doi: 10.1080/17512433.2020.1702025. [Epub ahead of print] PubMed PMID: 31810398.

2: de Almeida Carvalho LM, de Oliveira Sapori Avelar S, Haslam A, Gill J, Prasad V. Estimation of Percentage of Patients With Fibroblast Growth Factor Receptor Alterations Eligible for Off-label Use of Erdafitinib. JAMA Netw Open. 2019 Nov 1;2(11):e1916091. doi: 10.1001/jamanetworkopen.2019.16091. PubMed PMID: 31755953.

3: Dosne AG, Valade E, Stuyckens K, Li LY, Ouellet D, Perez-Ruixo JJ. Population Pharmacokinetics of Total and Free Erdafitinib in Adult Healthy Volunteers and Cancer Patients: Analysis of Phase 1 and Phase 2 Studies. J Clin Pharmacol. 2019 Nov 19. doi: 10.1002/jcph.1547. [Epub ahead of print] PubMed PMID: 31742712.

4: Chang SS. Re: Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma. J Urol. 2019 Nov 11:10109701JU0000614704308269b. doi: 10.1097/01.JU.0000614704.30826.9b. [Epub ahead of print] PubMed PMID: 31710554.

5: Poggesi I, Li LY, Jiao J, Hellemans P, Rasschaert F, de Zwart L, Snoeys J, De Meulder M, Mamidi RNVS, Ouellet D. Effect of Fluconazole and Itraconazole on the Pharmacokinetics of Erdafitinib in Healthy Adults: A Randomized, Open-Label, Drug-Drug Interaction Study. Eur J Drug Metab Pharmacokinet. 2019 Oct 31. doi: 10.1007/s13318-019-00581-9. [Epub ahead of print] PubMed PMID: 31673875.

6: Loriot Y, Necchi A, Siefker-Radtke AO. Erdafitinib in Urothelial Carcinoma. Reply. N Engl J Med. 2019 Oct 17;381(16):1594-1595. doi: 10.1056/NEJMc1911187. PubMed PMID: 31618553.

7: Sonpavde G, Sjödahl G. Erdafitinib in Urothelial Carcinoma. N Engl J Med. 2019 Oct 17;381(16):1594. doi: 10.1056/NEJMc1911187. PubMed PMID: 31618552.

8: Sharma V, Vanidassane I. Erdafitinib in Urothelial Carcinoma. N Engl J Med. 2019 Oct 17;381(16):1593-1594. doi: 10.1056/NEJMc1911187. PubMed PMID: 31618551.

9: Li LY, Guo Y, Gonzalez M, Ouellet D. Effect of Plasma Protein Binding on the Pharmacokinetics of Erdafitinib: Results of an Integrated Cross-Study Analysis. J Clin Pharmacol. 2019 Oct 10. doi: 10.1002/jcph.1529. [Epub ahead of print] PubMed PMID: 31602692.

10: Marandino L, Raggi D, Giannatempo P, Farè E, Necchi A. Erdafitinib for the treatment of urothelial cancer. Expert Rev Anticancer Ther. 2019 Oct;19(10):835-846. doi: 10.1080/14737140.2019.1671190. Epub 2019 Oct 4. PubMed PMID: 31544541.

11: Hanna KS. Erdafitinib to treat urothelial carcinoma. Drugs Today (Barc). 2019 Aug;55(8):495-501. doi: 10.1358/dot.2019.55.8.3010573. Review. PubMed PMID: 31461086.

12: Burki TK. Erdafitinib for advanced urothelial carcinoma. Lancet Oncol. 2019 Sep;20(9):e469. doi: 10.1016/S1470-2045(19)30522-4. Epub 2019 Aug 1. PubMed PMID: 31378458.

13: Loriot Y, Necchi A, Park SH, Garcia-Donas J, Huddart R, Burgess E, Fleming M, Rezazadeh A, Mellado B, Varlamov S, Joshi M, Duran I, Tagawa ST, Zakharia Y, Zhong B, Stuyckens K, Santiago-Walker A, De Porre P, O'Hagan A, Avadhani A, Siefker-Radtke AO; BLC2001 Study Group. Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma. N Engl J Med. 2019 Jul 25;381(4):338-348. doi: 10.1056/NEJMoa1817323. PubMed PMID: 31340094.

14: Valade E, Dosne AG, Xie H, Kleiman R, Li LY, Perez-Ruixo JJ, Ouellet D. Assessment of the effect of erdafitinib on cardiac safety: analysis of ECGs and exposure-QTc in patients with advanced or refractory solid tumors. Cancer Chemother Pharmacol. 2019 Sep;84(3):621-633. doi: 10.1007/s00280-019-03896-1. Epub 2019 Jul 6. PubMed PMID: 31280362.

15: Markham A. Erdafitinib: First Global Approval. Drugs. 2019 Jun;79(9):1017-1021. doi: 10.1007/s40265-019-01142-9. PubMed PMID: 31161538.

16: Bahleda R, Italiano A, Hierro C, Mita A, Cervantes A, Chan N, Awad M, Calvo E, Moreno V, Govindan R, Spira A, Gonzalez M, Zhong B, Santiago-Walker A, Poggesi I, Parekh T, Xie H, Infante J, Tabernero J. Multicenter Phase I Study of Erdafitinib (JNJ-42756493), Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients with Advanced or Refractory Solid Tumors. Clin Cancer Res. 2019 Aug 15;25(16):4888-4897. doi: 10.1158/1078-0432.CCR-18-3334. Epub 2019 May 14. PubMed PMID: 31088831.

17: Erdafitinib Efficacious in Bladder Cancer. Cancer Discov. 2018 Aug;8(8):OF6. doi: 10.1158/2159-8290.CD-NB2018-085. Epub 2018 Jun 27. PubMed PMID: 29950346.

18: Nishina T, Takahashi S, Iwasawa R, Noguchi H, Aoki M, Doi T. Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors. Invest New Drugs. 2018 Jun;36(3):424-434. doi: 10.1007/s10637-017-0514-4. Epub 2017 Sep 30. PubMed PMID: 28965185.

19: Karkera JD, Cardona GM, Bell K, Gaffney D, Portale JC, Santiago-Walker A, Moy CH, King P, Sharp M, Bahleda R, Luo FR, Alvarez JD, Lorenzi MV, Platero SJ. Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib. Mol Cancer Ther. 2017 Aug;16(8):1717-1726. doi: 10.1158/1535-7163.MCT-16-0518. Epub 2017 Apr 17. PubMed PMID: 28416604.

20: Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV. Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor. Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24. PubMed PMID: 28341788.