Infigratinib phosphate
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.
For research use only. We do not sell to patients.
- Purity: 99.19%
- CAS No.: 1310746-10-1
- Formula: C26H34Cl2N7O7P
- Molecular Weight:658.47
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Infigratinib phosphate
More- Signal Transduct Target Ther. 2025 Nov 3;10(1):360. [Abstract]
- Signal Transduct Target Ther. 2025 Nov 4;10(1):361. [Abstract]
- Nature. 2022 Aug;608(7923):609-617. [Abstract]
- Cancer Discov. 2019 Dec;9(12):1686-1695. [Abstract]
- Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
- Ann Rheum Dis. 2016 May;75(5):883-90. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2022 Aug 4;13(1):4534. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Exp Clin Cancer Res. 2021 Aug 27;40(1):273. [Abstract]
- J Control Release. 2018 Sep 28:286:254-263. [Abstract]
- Cell Death Dis. 2025 Jul 2;16(1):485. [Abstract]
- J Neuroinflammation. 2023 Jan 17;20(1):10. [Abstract]
- NPJ Precis Oncol. 2021 Jul 16;5(1):66. [Abstract]
- Oncogene. 2016 Apr 28;35(17):2247-65. [Abstract]
- Cell Rep. 2024 Dec 30;44(1):115116. [Abstract]
- Cell Rep. 2019 Feb 12;26(7):1709-1717.e3. [Abstract]
- J Med Chem. 2025 Mar 13;68(5):5907-5925. [Abstract]
- Pharmaceutics. 2025 Oct 31;17(11):1415. [Abstract]
- Cell Mol Life Sci. 2025 Nov 22. [Abstract]
- RSC Adv. 2020 Apr 23;10(28):16231-16244. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Oct;1871(7):167940. [Abstract]
- Obesity (Silver Spring). 2019 Mar;27(3):399-408. [Abstract]
- Sci Rep. 2016 Apr 28:6:25272. [Abstract]
- Cancers (Basel). 2024 Jul 3;16(13):2447. [Abstract]
- Biomedicines. 2023 Nov 27;11(12):3155. [Abstract]
- Chem Res Toxicol. 2021 Jul 19;34(7):1800-1813. [Abstract]
- Development. 2025 May 15;152(10):dev204687. [Abstract]
- Biotechnol J. 2024 Aug;19(8):e2400278. [Abstract]
- Peptides. 2026 Jan:195:171463. [Abstract]
- Tissue Eng Part A. 2019 Mar;25(5-6):437-445. [Abstract]
- FEBS Open Bio. 2023 May;13(5):804-817. [Abstract]
- Thorac Cancer. 2025 Jan;16(1):e15488. [Abstract]
- Anticancer Drugs. 2023 Oct 1;34(9):1035-1045. [Abstract]
- SSRN. 2026 May 20.
- bioRxiv. 2025 Nov 14:2025.11.14.680268. [Abstract]
- Biomed Pharmacother. 2025 Nov:192:118677. [Abstract]
- University of Auckland. 2025.
- Res Sq. 2025 Jul 24.
- bioRxiv. 2025 Jun 16:2025.06.11.659120. [Abstract]
- World J Exp Med. 2025 Jun 20;15(2):100443. [Abstract]
- bioRxiv. 2024 Oct 1:2024.05.12.593765. [Abstract]
- Heliyon. 2024 May 10;10(10):e31112. [Abstract]
- medRxiv. 2023 Mar 17.
- Patent. US20220175722A1.
- The 22nd National Graduate Research Conference. 2021 Mar 25.
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- Tag der mündlichen Prüfung. 2016.
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WB
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Flow Cytometry
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RT-PCR
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IF
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WB
Biological Activity
|
FGFR1 0.9 nM (IC50) |
FGFR2 1.4 nM (IC50) |
FGFR3 1 nM (IC50) |
FGFR4 60 nM (IC50) |
|
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] |
Infigratinib phosphate inhibits FGFR1, FGFR2, and FGFR3 with IC50=~1 nM, FGFR3K650E 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1310746-10-1
-
Appearance Solid
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Molecular Weight 658.47
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Formula C26H34Cl2N7O7P
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Color White to gray
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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
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Synonyms
BGJ-398 phosphate; NVP-BGJ398 phosphate
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
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
-
Most Recent
-
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
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.
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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
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.
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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).
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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
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
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
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
2026 Jan:195:171463. PMID: 41485715 -
Tissue Eng Part A
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 -
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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 -
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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
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 -
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (37.97 mM); Suspended solution; Need ultrasonic
Protocol
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.
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.
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.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |