Erdafitinib (JNJ-42756493)

製品コードS8401 バッチS840103

印刷

化学情報

Synonyms

JNJ-42756493

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₅H₃₀N₆O₂

分子量

446.54

CAS No.

1346242-81-6

Solubility (25°C)*

体外

DMSO

89 mg/mL (199.31 mM)

Ethanol

89 mg/mL (199.31 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
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 this compound is decreased, associated with increased apoptotic death and decreased cell survival^[2].
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]. This compound shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. It 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].

プロトコル(参考用のみ)

細胞アッセイ	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.
動物実験	動物モデル	NMRI nu/nu female mice
	投薬量	40 mg/kg
	投与方法	by gavage

参考

http://cancerres.aacrjournals.org/content/74/19_Supplement/1738.short
https://pubmed.ncbi.nlm.nih.gov/26675289/
https://pubmed.ncbi.nlm.nih.gov/31461086/

カスタマーフィードバック

: , , Clin Cancer Res, 2017, 23(18):5527-5536

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Single-cell analysis reveals transcriptomic features and therapeutic targets in primary pulmonary lymphoepithelioma-like carcinoma [ Commun Biol, 2025, 8(1):394]	PubMed: 40057671
Using Cancer-Associated Fibroblasts as a Shear-Wave Elastography Imaging Biomarker to Predict Anti-PD-1 Efficacy of Triple-Negative Breast Cancer [ Int J Mol Sci, 2025, 26(8)3525]	PubMed: 40332007
FGFR inhibition augments anti-PD-1 efficacy in murine FGFR3-mutant bladder cancer by abrogating immunosuppression [ J Clin Invest, 2024, 134(2)e169241]	PubMed: 38226620
Chromatin Remodeling in Patient-Derived Colorectal Cancer Models [ Adv Sci (Weinh), 2024, 11(16):e2303379]	PubMed: 38380561
Understanding and Overcoming Resistance to Selective FGFR inhibitors Across FGFR2-Driven Malignancies [ Clin Cancer Res, 2024, 10.1158/1078-0432.CCR-24-1834]	PubMed: 39226398
FGF receptor kinase inhibitors exhibit broad antiviral activity by targeting Src family kinases [ Cell Mol Life Sci, 2024, 81(1):471]	PubMed: 39621133
Targeting metabolic reprogramming to overcome drug resistance in advanced bladder cancer: insights from gemcitabine- and cisplatin-resistant models [ Mol Oncol, 2024, 10.1002/1878-0261.13684]	PubMed: 38874588
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011]	PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011]	PubMed: 37377403

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。