製品番号: HY-13311A

Infigratinib phosphate

(別名: BGJ-398 phosphate; NVP-BGJ398 phosphate)

48 Cited Publications

カスタマーレビュー

Based on 48 publication(s) in Google Scholar

Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC₅₀ of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.19%
CAS 番号: 1310746-10-1
分子式: C₂₆H₃₄Cl₂N₇O₇P
分子量:658.47

保管条件:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Infigratinib phosphate 構造式

CAS 番号: 1310746-10-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (48)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

FGFR1

0.9 nM (IC₅₀)

FGFR2

1.4 nM (IC₅₀)

FGFR3

1 nM (IC₅₀)

FGFR4

60 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.7 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR3 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of FGFR3 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	1449 nM Compound: 1h, NVP-BGJ398	Inhibition of VEGFR2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of VEGFR2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	1510 nM Compound: 1h, NVP-BGJ398	Inhibition of VEGFR1 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of VEGFR1 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	1857 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against mouse wild type BAF3 cells assessed as decrease in cell viability by luminescence-based assay Antiproliferative activity against mouse wild type BAF3 cells assessed as decrease in cell viability by luminescence-based assay	[PMID: 21936542]
BaF3	IC₅₀	2 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against mouse BAF3 cell line transformed with TEL-FGFR3 construct after 48 hrs by luciferase bioluminescent assay Antiproliferative activity against mouse BAF3 cell line transformed with TEL-FGFR3 construct after 48 hrs by luciferase bioluminescent assay	[PMID: 21936542]
BaF3	IC₅₀	2 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR2 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of FGFR2 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR3-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of FGFR3-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2.9 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR1-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of FGFR1-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2051 nM Compound: 1h, NVP-BGJ398	Inhibition of TIE2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of TIE2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2072 nM Compound: 1h, NVP-BGJ398	Inhibition of VEGFR3 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of VEGFR3 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2192 nM Compound: 1h, NVP-BGJ398	Inhibition of BCR-ABL-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of BCR-ABL-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2482 nM Compound: 1h, NVP-BGJ398	Inhibition of LCK-B-mediated proliferation of mouse BAF3 cells transformed with Tel-kinase construct Inhibition of LCK-B-mediated proliferation of mouse BAF3 cells transformed with Tel-kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2501 nM Compound: 1h, NVP-BGJ398	Inhibition of KIT juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of KIT juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2718 nM Compound: 1h, NVP-BGJ398	Inhibition of PDGFRalpha-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of PDGFRalpha-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2882 nM Compound: 1h, NVP-BGJ398	Inhibition of JAK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of JAK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2891 nM Compound: 1h, NVP-BGJ398	Inhibition of RON-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of RON-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	2969 nM Compound: 1h, NVP-BGJ398	Inhibition of SRC-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of SRC-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3011 nM Compound: 1h, NVP-BGJ398	Inhibition of MET-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of MET-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3019 nM Compound: 1h, NVP-BGJ398	Inhibition of LYN-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of LYN-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3039 nM Compound: 1h, NVP-BGJ398	Inhibition of EPHB1-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of EPHB1-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3078 nM Compound: 1h, NVP-BGJ398	Inhibition of ALK juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of ALK juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3139 nM Compound: 1h, NVP-BGJ398	Inhibition of TRKB juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of TRKB juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3252 nM Compound: 1h, NVP-BGJ398	Inhibition of FLT3-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of FLT3-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3263 nM Compound: 1h, NVP-BGJ398	Inhibition of ROS-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of ROS-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3303 nM Compound: 1h, NVP-BGJ398	Inhibition of TYK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of TYK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3352 nM Compound: 1h, NVP-BGJ398	Inhibition of RET juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of RET juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3371 nM Compound: 1h, NVP-BGJ398	Inhibition of INSR-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of INSR-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	3405 nM Compound: 1h, NVP-BGJ398	Inhibition of BMX-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of BMX-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	4142 nM Compound: 1h, NVP-BGJ398	Inhibition of B-RAF V600E mutant-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of B-RAF V600E mutant-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	52.2 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR3 K650E mutant-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of FGFR3 K650E mutant-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	5358 nM Compound: 1h, NVP-BGJ398	Inhibition of SYK-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of SYK-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
BaF3	IC₅₀	938 nM Compound: 1h, NVP-BGJ398	Inhibition of VEGFR2 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct Inhibition of VEGFR2 juxtamembrane domain-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct	[PMID: 21936542]
HEK293	IC₅₀	168 nM Compound: 1h, NVP-BGJ398	Inhibition of wild type FGFR4 expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay Inhibition of wild type FGFR4 expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay	[PMID: 21936542]
HEK293	IC₅₀	4.6 nM Compound: 1h, NVP-BGJ398	Inhibition of wild type FGFR1 expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay Inhibition of wild type FGFR1 expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay	[PMID: 21936542]
HEK293	IC₅₀	4.9 nM Compound: 1h, NVP-BGJ398	Inhibition of wild type FGFR2 expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay Inhibition of wild type FGFR2 expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay	[PMID: 21936542]
HEK293	IC₅₀	5 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR3 K650E mutant expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay Inhibition of FGFR3 K650E mutant expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay	[PMID: 21936542]
HEK293	IC₅₀	5 nM Compound: 1h, NVP-BGJ398	Inhibition of FGFR3 S249C mutant expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay Inhibition of FGFR3 S249C mutant expressed in HEK293 cells assessed as inhibition of autophosphorylation of tyrosine residue after 40 mins by ELISA assay	[PMID: 21936542]
HT1197	IC₅₀	1157 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human HT1197 cells after 72 hrs Antiproliferative activity against human HT1197 cells after 72 hrs	[PMID: 21936542]
J82	IC₅₀	>3000 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human J82 cells after 72 hrs Antiproliferative activity against human J82 cells after 72 hrs	[PMID: 21936542]
RT-112	IC₅₀	5 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human RT112 cells overexpressing wild type FGFR3 after 72 hrs Antiproliferative activity against human RT112 cells overexpressing wild type FGFR3 after 72 hrs	[PMID: 21936542]
RT-4	IC₅₀	30 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human RT4 cells overexpressing wild type FGFR3 after 72 hrs Antiproliferative activity against human RT4 cells overexpressing wild type FGFR3 after 72 hrs	[PMID: 21936542]
SW780	IC₅₀	32 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human SW780 cells overexpressing wild type FGFR3 after 72 hrs Antiproliferative activity against human SW780 cells overexpressing wild type FGFR3 after 72 hrs	[PMID: 21936542]
UMUC3	IC₅₀	>3000 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human UM-UC-3 cells after 72 hrs Antiproliferative activity against human UM-UC-3 cells after 72 hrs	[PMID: 21936542]
VM-CUB-1	IC₅₀	>3000 nM Compound: 1h, NVP-BGJ398	Antiproliferative activity against human VMCUB1 cells after 72 hrs Antiproliferative activity against human VMCUB1 cells after 72 hrs	[PMID: 21936542]

体外実験

Infigratinib phosphate inhibits FGFR1, FGFR2, and FGFR3 with IC₅₀=~1 nM, FGFR3^K650E with IC₅₀=4.9 nM, and FGFR4 with IC₅₀=60 nM. IC₅₀ values for all other kinases are in the μM range (FYN, LCK, YES, and ABL, IC₅₀=1.9, 2.5, 1.1, and 2.3 μM, respectively) except for VEGFR2, KIT, and LYN, which are inhibited at submicromolar concentrations (IC₅₀=0.18, 0.75, and 0.3 μM, respectively). Infigratinib inhibits the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC₅₀ values which are in the low nanomolar range and comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay. For the remaining cells, all IC₅₀ values are greater than 1.5 μM except for VEGFR2 (IC₅₀ 1449 and 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, and FGFR3^[1]. Infigratinib (ranging between 1 nM and 10 μM) is potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Infigratinib is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5 mg/kg intravenous bolus in NMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20 mg/kg dose. The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. After intravenous dosing, Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues, translating into a high volume of distribution (26 L/kg). The plasma clearance is high at 3.3 L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10^[1]. Infigratinib (30 mg/kg) significantly inhibits the growth of FGFR2-mutated endometrial cancer xenograft models^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1310746-10-1
性状 Solid
分子量 658.47
分子式 C₂₆H₃₄Cl₂N₇O₇P
Color White to gray
SMILES

O=P(O)(O)O.ClC1=C(C(Cl)=C(C=C1OC)OC)NC(N(C2=CC(NC3=CC=C(C=C3)N4CCN(CC4)CC)=NC=N2)C)=O
別名

BGJ-398 phosphate; NVP-BGJ398 phosphate
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Publications (48)

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Journal Impact Factor

Signal Transduct Target Ther

Microglia-derived nanovesicles synchronize macroautophagy and chaperone-mediated autophagy for Alzheimer's disease therapy. [Abstract]

2025 Nov 3;10(1):360. PMID: 41184271
Signal Transduct Target Ther

Olverembatinib, a multikinase inhibitor that modulates lipid metabolism, in advanced succinate dehydrogenase-deficient gastrointestinal stromal tumors: a phase 1b study and translational research. [Abstract]

2025 Nov 4;10(1):361. PMID: 41184234
Nature

Truncated FGFR2 is a clinically actionable oncogene in multiple cancers. [Abstract]

2022 Aug;608(7923):609-617. PMID: 35948633
Cancer Discov

Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma. [Abstract]

2019 Dec;9(12):1686-1695. PMID: 31575540
Cancer Discov

Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer. [Abstract]

2018 Mar;8(3):354-369. PMID: 29203461

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]

BGJ398 (30-50 mg/kg; oral). In vivo dosing of BGJ398 at 30mg/kg achieves target inhibition measured by pFrs2 and pErk levels.

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]

BGJ398 (30-50 mg/kg; oral). Combining BGJ398 and a different PARP-inhibitor, BMN673, induces sustained tumor remission.
Ann Rheum Dis

Nintedanib inhibits fibroblast activation and ameliorates fibrosis in preclinical models of systemic sclerosis. [Abstract]

2016 May;75(5):883-90. PMID: 25858641
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Accurate determination of CRISPR-mediated gene fitness in transplantable tumours. [Abstract]

2022 Aug 4;13(1):4534. PMID: 35927228
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Exp Clin Cancer Res

Cyclin G2 reverses immunosuppressive tumor microenvironment and potentiates PD-1 blockade in glioma. [Abstract]

2021 Aug 27;40(1):273. PMID: 34452627

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Aug 27;40(1):273. [Abstract]

BGJ398 (10 nM; 24 h). Western blotting was performed to examine the effect of cyclin G2 on Y10 phosphorylation of LDHA in the presence or absence of BGJ398.
J Control Release

New path to treating pancreatic cancer: TRAIL gene delivery targeting the fibroblast-enriched tumor microenvironment. [Abstract]

2018 Sep 28:286:254-263. PMID: 30075209
Cell Death Dis

FGFR inhibitors promote the autophagic degradation of IFN-γ-induced PD-L1 and alleviate the PD-L1-mediated transcriptional suppression of FGFR3-TACC3 in non-muscle-invasive bladder cancer. [Abstract]

2025 Jul 2;16(1):485. PMID: 40603902

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jul 2;16(1):485. [Abstract]

BGJ398 (0-80 nM; 48 h). RT4 cells were treated with vehicle control or the indicated concentrations of BGJ398 in the presence or absence of interferon (IFN)-γ (10 ng/ml) for 48 h and subjected to western blot analysis.

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jul 2;16(1):485. [Abstract]

RT-112 cells were exposed to IFN-γ (10 ng/ml) with or without L145 (2 μM) or BGJ398 (0.08 μM) for 48 h, stained with αPD-L1 antibody, and subjected to flow cytometry analysis.

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jul 2;16(1):485. [Abstract]

BGJ398 (0.04 μM; 6-48 h). RT-112 cells were treated with vehicle control (CTRL) or IFN-γ (10 ng/ml) with or without L145 (1 μM) or BGJ398 (0.04 μM) for the indicated times, and subjected to RT-qPCR analyses.

Infigratinib phosphate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jul 2;16(1):485. [Abstract]

RT-112 cells were treated with interferon (IFN)-γ (10 ng/ml) alone or in combination with L145 (1 μM) or BGJ398 (0.08 μM) for 24 h and subjected to immunofluorescence staining with antibodies against PD-L1 (green) and LC3B (red).
J Neuroinflammation

The FGF/FGFR system in the microglial neuroinflammation with Borrelia burgdorferi: likely intersectionality with other neurological conditions. [Abstract]

2023 Jan 17;20(1):10. PMID: 36650549
NPJ Precis Oncol

Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer. [Abstract]

2021 Jul 16;5(1):66. PMID: 34272467
Oncogene

YAP induces high-grade serous carcinoma in fallopian tube secretory epithelial cells. [Abstract]

2016 Apr 28;35(17):2247-65. PMID: 26364602
Cell Rep

IMPDH2 dephosphorylation under FGFR signaling promotes S-phase progression and tumor growth. [Abstract]

2024 Dec 30;44(1):115116. PMID: 39739531
Cell Rep

Germline Stem Cells Drive Ovary Regeneration in Zebrafish. [Abstract]

2019 Feb 12;26(7):1709-1717.e3. PMID: 30759383
J Med Chem

Discovery of Novel 2,4,5-Trisubstituted Pyrimidine Derivatives as Potent and Selective FGFR Inhibitors against Gatekeeper Mutants for the Treatment of NSCLC. [Abstract]

2025 Mar 13;68(5):5907-5925. PMID: 40032550
Pharmaceutics

8-Hydroxy-2-Anilino-1,4-Naphthoquinone Prevents Against Ferroptotic Neuronal Death and Kainate-Induced Epileptic Seizures. [Abstract]

2025 Oct 31;17(11):1415. PMID: 41304754
Cell Mol Life Sci

ALKBH5 demethylation modification of SE-lncRNA ZMIZ1-AS1 promotes FGFR1-mediated proliferation and invasive metastasis in osteosarcoma. [Abstract]

2025 Nov 22. PMID: 41275058
RSC Adv

Identification and characterization of in silico, in vivo, in vitro, and reactive metabolites of infigratinib using LC-ITMS: bioactivation pathway elucidation and in silico toxicity studies of its metabolites. [Abstract]

2020 Apr 23;10(28):16231-16244. PMID: 35498820
Biochim Biophys Acta Mol Basis Dis

Combined inhibition of EGFR and FGFRs with Cetuximab and Infigratinib showed effectiveness and relevance in proliferation and migration of HNSCC cell lines. [Abstract]

2025 Oct;1871(7):167940. PMID: 40449758
Obesity (Silver Spring)

Fibroblast Growth Factor 21 Exerts its Anti-inflammatory Effects on Multiple Cell Types of Adipose Tissue in Obesity. [Abstract]

2019 Mar;27(3):399-408. PMID: 30703283
Sci Rep

Up-regulation of FGFBP1 signaling contributes to miR-146a-induced angiogenesis in human umbilical vein endothelial cells. [Abstract]

2016 Apr 28:6:25272. PMID: 27121396
Cancers (Basel)

TMEM176B Promotes EMT via FGFR/JNK Signalling in Development and Tumourigenesis of Lung Adenocarcinoma. [Abstract]

2024 Jul 3;16(13):2447. PMID: 39001509
Biomedicines

Tephrosin Suppresses the Chemoresistance of Paclitaxel-Resistant Ovarian Cancer via Inhibition of FGFR1 Signaling Pathway. [Abstract]

2023 Nov 27;11(12):3155. PMID: 38137377
Chem Res Toxicol

Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib. [Abstract]

2021 Jul 19;34(7):1800-1813. PMID: 34189909
Development

Specific mitotic events drive left-right organizer development. [Abstract]

2025 May 15;152(10):dev204687. PMID: 40230260
Biotechnol J

Discovery of fibroblast growth factor 2-derived peptides for enhancing mice skeletal muscle satellite cell proliferation. [Abstract]

2024 Aug;19(8):e2400278. PMID: 39212202
Peptides

FGF9 drives mitochondrial biogenesis in glioblastoma by activating the CREB-PGC-1α axis. [Abstract]

2026 Jan:195:171463. PMID: 41485715
Tissue Eng Part A

Integration Capacity of Human Induced Pluripotent Stem Cell-Derived Cartilage. [Abstract]

2019 Mar;25(5-6):437-445. PMID: 30129877
FEBS Open Bio

Reduced FRG1 expression promotes angiogenesis via activation of the FGF2-mediated ERK/AKT pathway. [Abstract]

2023 May;13(5):804-817. PMID: 36815234
Thorac Cancer

Establishing a new human lung squamous cell carcinoma cell line, OMUL-1, expressing insulin-like growth factor 1 receptor and programmed cell death ligand 1. [Abstract]

2025 Jan;16(1):e15488. PMID: 39552203
Anticancer Drugs

Derazantinib, a fibroblast growth factor receptor inhibitor, inhibits colony-stimulating factor receptor-1 in macrophages and tumor cells and in combination with a murine programmed cell death ligand-1-antibody activates the immune environment of murine syngeneic tumor models. [Abstract]

2023 Oct 1;34(9):1035-1045. PMID: 36729099
SSRN

2026 May 20.
bioRxiv

Disruption of the FGFR1-FGF23-Phosphate Axis and Targeted Therapy in a Murine Model of Osteoglophonic Dysplasia. [Abstract]

2025 Nov 14:2025.11.14.680268. PMID: 41473314
Biomed Pharmacother

FGF/FGFR inhibitors downmodulates c-Myc oncoprotein and hampers the growth of adrenocortical carcinoma. [Abstract]

2025 Nov:192:118677. PMID: 41124865
University of Auckland

2025.
Res Sq

2025 Jul 24.
bioRxiv

A Hotspot Phosphorylation Site on SHP2 Drives Oncoprotein Activation and Drug Resistance. [Abstract]

2025 Jun 16:2025.06.11.659120. PMID: 40667115
World J Exp Med

Establishment and characterization of a new human gallbladder cancer cell line, OCUG-2. [Abstract]

2025 Jun 20;15(2):100443. PMID: 40546672
bioRxiv

Specific Mitotic Events Drive Cytoskeletal Remodeling Required for Left-Right Organizer Development. [Abstract]

2024 Oct 1:2024.05.12.593765. PMID: 38798489
Heliyon

Dual blockage of PI3K-mTOR and FGFR induced autophagic cell death in cholangiocarcinoma cells. [Abstract]

2024 May 10;10(10):e31112. PMID: 38799762
medRxiv

2023 Mar 17.
Patent

US20220175722A1.
The 22nd National Graduate Research Conference

2021 Mar 25.
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841
Tag der mündlichen Prüfung

2016.

溶剤 & 溶解度

体外:

DMSO : 8.75 mg/mL (13.29 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5187 mL

7.5934 mL

15.1867 mL

5 mM

0.3037 mL

1.5187 mL

3.0373 mL

10 mM

0.1519 mL

0.7593 mL

1.5187 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 25 mg/mL (37.97 mM); Suspended solution; Need ultrasonic

プロトコル

Kinase Assay^[1]

The enzymatic kinase activity is assessed by measuring the phosphorylation of a synthetic substrate by the purified GST-fusion FGFR3-K650E kinase domain, in the presence of radiolabeled ATP. Enzyme activities are measured by mixing 10 μL of a 3-fold concentrated Infigratinib solution or control with 10 μL of the corresponding substrate mixture (peptidic substrate, ATP and [γ³³P]ATP). The reactions are initiated by addition of 10 μL of a 3-fold concentrated solution of the enzyme in assay buffer. The final concentrations of the assay components are as following: 10 ng of GST-FGFR3-K650E, 20 mM Tris-HCl, pH 7.5, 3 mM MnCl₂, 3 mM MgCl₂, 1 mM DTT, 250 μg/mL PEG 20000, 2 μg/mL poly(EY) 4:1, 1% DMSO and 0.5 μM ATP (γ-[³³P]-ATP 0.1 μCi). The assay is carried out according to the filter binding (FB) method in 96-well plates at room temperature for 10 min in a final volume of 30 μL including the components as indicated above. The enzymatic reactions are stopped by the addition of 20 μL of 125 mM EDTA, and the incorporation of ³³P into the polypeptidic substrates is quantified as following: 30 μL of the stopped reaction mixture are transferred onto Immobilon-PVDF membranes previously soaked for 5 min with methanol, rinsed with water, soaked for 5 min with 0.5% H₃PO₄, and mounted on vacuum manifold with disconnected vacuum source. After spotting, vacuum is connected, and each well rinsed with 0.5% H₃PO₄ (200 μL). Free membranes are removed and washed four times on a shaker with 1% H₃PO₄ and once with ethanol. Membranes are dried and overlaid with addition of 10 μL/well of a scintillation fluid. The plates are eventually sealed and counted in a microplate scintillation counter. IC₅₀ values are calculated by linear regression analysis of the percentage inhibition of NVP-BGJ398^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Murine BaF3 cell lines are cultured in RPMI-1640 media supplemented with 10% FBS, 4.5 g/L glucose, 1.5 g/L sodium bicarbonate, and Pen/Strep. Cells are passaged twice weekly. Compound-mediated inhibition of BaF3 cell proliferation and viability is assessed using a Luciferase bioluminescent assay. Exponentially growing BaF3 or BaF3 Tel-TK cells are seeded into 384-well plates (4250 cells/well) at 50 μL/well using a μFill liquid dispenser in fresh medium. Infigratinib is serially diluted in DMSO and arrayed in a polypropylene 384-well plate. Then 50 nL of compound are transferred into the plates containing the cells by using the pintool transfer device, and the plates incubated at 37°C (5% CO₂) for 48 h. Then 25 μL of Bright-Glo are added, and luminescence is quantified using an Analyst-GT. Custom curve-fitting software is used to produce a logistic fit of percent cell viability as a function of the logarithm of inhibitor concentration. The IC₅₀ value is determined as the concentration of compound needed to reduce cell viability to 50% of a DMSO control^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Female HsdNpa: Athymic Nude-nu mice are used. Infigratinib is formulated as a suspension in PEG300/D5W (2:1, v/v) and administered orally for 12 consecutive days at the doses of 10 and 30 mg/kg/qd. Tumor and body weight data are analyzed by ANOVA with post hoc Dunnett’s test for comparison of treatment versus control group. The post hoc Tukey test is used for intragroup comparison. Statistical analysis is performed using GraphPad prism 4.02. As a measure of efficacy, the T/C (%) value is calculated.
Rats^[1]
Female nude Rowett rats 6-9 weeks of age are used. Infigratinib is formulated as a solution in acetic acid-acetate buffer pH 4.6/PEG300 (1:1, v/v) and applied daily by gavage to the tumor-bearing rats (n=8) for 20 consecutive days at doses of 5, 10, and 15 mg/kg/qd (free base equivalents). The application volume is 5 mL/kg. Tumor volumes are measured with calipers and determined according to the formula: length×width×height×π/6. Antitumor activity is expressed as T/C (%): (mean change of tumor volume of treated animals/mean change of tumor volume of control animals)×100. Regressions (%) are calculated.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Guagnano V, et al. Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-me thyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor T [Content Brief]

[2]. Konecny GE, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5187 mL	7.5934 mL	15.1867 mL	37.9668 mL
	5 mM	0.3037 mL	1.5187 mL	3.0373 mL	7.5934 mL
	10 mM	0.1519 mL	0.7593 mL	1.5187 mL	3.7967 mL

Keywords

Infigratinib phosphate

48 Cited Publications

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Infigratinib phosphate

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MedChemExpress（MCE）の使用を引用している文献 Infigratinib phosphate

生物活性

化学情報

Publications (48)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Infigratinib phosphate 関連分類

HY-13311A 関連分類