Erdafitinib

Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.

CAS No. 1346242-81-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 59500	国内在庫あり
100mg	JPY 145500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（32）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

Erdafitinibと併用されることが多い化合物

Pemigatinib

Erdafitinib and Pemigatinib are approved by FDA for their use in the treatment of FGFR3-mutated urothelial carcinoma and FGFR2-fusion cholangiocarcinoma, respectively.

Krook MA, et al. Br J Cancer. 2021 Mar;124(5):880-892.

Alpelisib (BYL719)

Erdafitinib and Alpelisib combined with the canonical cytotoxic agents result in variable synergistic, additive, and antagonistic effects in neuroblastoma (NB) cell lines.

Holzhauser S, et al. Int J Oncol. 2021 Feb;58(2):211-225.

Navitoclax (ABT-263)

Erdafitinib and Navitoclax induce potent apoptosis in urothelial carcinoma cell lines without FGFR mutation.

Ohtsu A, et al. Cancer Res (2021) 81 (13_Supplement): 1928.

Idasanutlin (RG7388)

Erdafitinib and Idasanutlin exert a synergistic effect on viability, apoptosis, and clonogenicity in one WDLPS and two DDLPS cell lines.

Dadone-Montaudie B, et al. Cancers (Basel). 2020 Oct 20;12(10):3058.

AZD4547

Erdafitinib and AZD4547 not only inhibit cell proliferation but also reduce the 18F-FDG uptake in NCI-H1581 cells.

Jiang Y, et al. Theranostics. 2022 Aug 29;12(14):6395-6408.

Erdafitinib関連製品

関連ターゲット	FGFR1 FGFR2 FGFR3 FGFR4	もっと見る
関連化合物ライブラリー	Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Angiogenesis Related compound Library HIF-1 Signaling Pathway Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

FGFRシグナル伝達経路

FGFR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
BA/F3	Function assay	24 hrs	Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed as decrease in cell proliferation in absence of mouse IL3 after 24 hrs by Alamar blue assay, IC50 = 0.01585 μM.	ChEMBL
BA/F3	Function assay	24 hrs	Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed as decrease in cell proliferation in absence of mouse IL3 after 24 hrs by Alamar blue assay, IC50 = 0.08318 μM.	ChEMBL
BA/F3	Function assay	24 hrs	Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed as decrease in cell proliferation in absence of mouse IL3 after 24 hrs by Alamar blue assay, IC50 = 3.31131 μM.	ChEMBL
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生物活性

製品説明

Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.

Targets

FGFR ^[1]

RET ^[3]

CSF-1R ^[3]

PDGFR ^[3]

Kit ^[3]

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In Vitro
In vitro	JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival^[2].
細胞実験	細胞株	HCT116, HCA7, Caco2 and NCI-H716 cells
	濃度	--
	反応時間	72 h
	実験の流れ	The effect of varying drug concentrations on cell growth and survival is evaluated at 72 h using sulforhodamine B (SRB) assay for the adherent cells (HCT116, HCA7, Caco2) and trypan blue dye exclusion for the suspension cells, NCI-H716.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	FGFR2 / p-FGFR PARP / Cleaved PARP / AKT / p-AKT / p-ERK / ERK2		26675289
	Growth inhibition assay	Cell viability		26675289

In Vivo
In Vivo	In vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control^[2]. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components^[1].
動物実験	動物モデル	NMRI nu/nu female mice
	投与量	40 mg/kg
	投与経路	by gavage

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05567185	Recruiting	Urinary Bladder Neoplasms\|Receptors Fibroblast Growth Factor	Janssen Pharmaceutical K.K.	March 3 2023	Phase 1
NCT05316155	Recruiting	Urinary Bladder Neoplasms\|Receptors Fibroblast Growth Factor	Janssen Research & Development LLC	April 11 2022	Phase 1
NCT05052372	Terminated	Bladder Cancer\|Urothelial Carcinoma\|Transitional Cell Carcinoma\|Platinum-Resistant Urothelial Carcinoma\|Bladder Urothelial Carcinoma\|FGFR Mutation\|FGFR2 Gene Mutation\|FGFR3 Gene Mutation\|FGFR2 Amplification\|Locally Advanced Urothelial Carcinoma\|Metastatic Urothelial Carcinoma\|Refractory Bladder Carcinoma\|Refractory Bladder Urothelial Carcinoma	xCures	November 21 2021	--
NCT04330248	Completed	Healthy	Johnson & Johnson Pharmaceutical Research & Development L.L.C.	March 31 2020	Phase 1
NCT04083976	Active not recruiting	Advanced Solid Tumor	Janssen Research & Development LLC	November 20 2019	Phase 2

参考
[1] Timothy Perera, et al. Cancer Res. 2014, 74(19 Suppl):Abstract nr 1738. [2] Verstraete M, et al. BMC Cancer. 2015, 15:946. [3] K S Hanna. Drugs Today (Barc). 2019 Aug;55(8):495-501.

参考

化学情報

分子量	446.54	化学式	C₂₅H₃₀N₆O₂
CAS No.	1346242-81-6	SDF	Download Erdafitinib SDFをダウンロードする
Smiles	CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 89 mg/mL ( (199.31 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 89 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):