BGJ398 (NVP-BGJ398|Infigratinib)

Catalog No.S2183

BGJ398 (NVP-BGJ398|Infigratinib) Chemical Structure

Molecular Weight(MW): 560.48

BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.

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Cited by 27 Publications

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Biological Activity

Description BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
Targets
FGFR1 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
FGFR3 (K650E) [1]
(Cell-free assay)
FGFR4 [1]
(Cell-free assay)
0.9 nM 1.0 nM 1.4 nM 4.9 nM 60 nM
In vitro

BGJ398 also prevents VEGFR2 with low potency. The IC50 of BGJ398 for inhibiting VEGFR2 is 0.18 μM. BGJ398 suppresses other kinases including ABL, FYN, KIT, LCK, LYN and YES with IC50 of 2.3 μM, 1.9 μM, 0.75 μM, 2.5 μM, 0.3 μM and 1.1 μM, respectively. At the cellular level, BGJ398 inhibits the proliferation of the FGFR1-, FGFR2-Q, and FGFR3-dependent BaF3 cells with IC50 of 2.9 μM, 2.0 μM and 2 μM, respectively. BGJ398 interferes with autophosphorylation on specific tyrosine residues including FGFR-WT, FGFR2-WT, FGFR3-K650E, FGFR3-S249C and FGFR4-WT with IC50 of 4.6 nM, 4.9 nM, 5 nM, 5 nM and 168 nM, respectively. BGJ398 suppresses proliferation of the cancer cells with wild-type (WT) FGFR3 overexpression such as RT112, RT4, SW780 and JMSU1 with IC50 of 5 nM, 30 nM, 32 nM and 15 nM, respectively. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorKNU0zPTByIH7N MmDmOFghcA>? NGfOVnXDqEmFNUC9JFI{PTokgJnucS=> NGG2XFIzPTZ6OEe0Ny=>
HCC M3;Lfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInKR|gyNTJ3MECgcm0> MnjDOFghcA>? M4\HPWlEPTB;MUGyOQKBkW6v M17aZVI2Pjh6N{Sz
HCT116 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHiOFghcA>? NVvHOHdZUUN3ME2zJO69VQ>? NYLCVXpxOjR3MEO1N|g>
HKH2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:0PEBp M2TqdGlEPTB;NDFOwG0> NVHQe4RPOjR3MEO1N|g>
RKO MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HLfVQ5KGh? MULJR|UxRTFwMjFOwG0> NH;Nd20zPDVyM{WzPC=>
LS174T NV3Lc2dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXHPIg1QCCq NGDSbVNKSzVyPUSg{txO M3;4VFI1PTB|NUO4
HCD9 NGf6PGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDVTJlFOC53LUWg{txO NUTKeIZwPDhxN{KgbC=> NIDNNmRFVVOR MlPp[IVkemWjc3XzJINmdGxidnnhZoltcXS7 MmXkNlQyOzV6MU[=
HCT116 NGO1foZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jDUVAvPS13IN88US=> NV3RXmpmPDhxN{KgbC=> M{XZNmROW09? MYnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? NYnxS2dbOjRzM{W4NVY>
SNU-C1 Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13keVAvPS13IN88US=> M3TK[VQ5Nzd{IHi= MXXEUXNQ NFjVc2VvdyCnZn\lZ5Q> M{DUbFI1OTN3OEG2
MFE280 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LQT2lEPTB;Mj62N{DDuSByLkiyJO69VQ>? MlfUNlM1PDN6MEW=
AN3CA M3fkV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfXTWM2OD1zLkCwJOKyKDBwMkCg{txO NXy4TppjOjN2NEO4NFU>
HEC155 NUPLN3lUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTRwN{SgxtEhOS5yOTFOwG0> MX6yN|Q1OzhyNR?=
MFE296 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHNSXd6UUN3ME2yMlg3KMLzIECuNlAh|ryP MUGyN|Q1OzhyNR?=
SPAC1S MkHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTNwMUmgxtEhOC57MzFOwG0> NFf6[FQzOzR2M{iwOS=>
RL952 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTDTWM2OD1|LkSxJOKyKDBwMkOg{txO MUCyN|Q1OzhyNR?=
EN1 MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnvO|Q1UUN3ME20Mlc2KMLzIECuOlIh|ryP NUTF[ZRlOjN2NEO4NFU>
SNGII NV;4VldST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTRwMkmgxtEhOC53ODFOwG0> MX6yN|Q1OzhyNR?=
ISHIKAWA M3rBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS4PYZbUUN3ME21MlQ5KMLzIECuNFMh|ryP Mm\sNlM1PDN6MEW=
HEC1A MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHS[VNKSzVyPUGwMlAxKMLzIEGuNFAh|ryP MX:yN|Q1OzhyNR?=
KLE Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jCdGlEPTB;Mz6wN{DDuSByLkGxJO69VQ>? NF7TW5IzOzR2M{iwOS=>
SNGM NVHCPZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1OwNmlEPTB;NT6wNEDDuSByLkSxJO69VQ>? NWDoSmREOjN2NEO4NFU>
USPC2 NFjtXJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHITWM2OD15LkCwJOKyKDBwMkGg{txO NX;PVpFPOjN2NEO4NFU>
EN NYPqPY1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7JZlhKSzVyPU[uNFMhyrFiMD6zNUDPxE1? NFT2OWQzOzR2M{iwOS=>
MFE319 Mn:wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDESYVKSzVyPUWuN|chyrFiMD6wN{DPxE1? M3zqd|I{PDR|OEC1
EFE184 M2PIdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRThwMESgxtEhOC54OTFOwG0> MmKyNlM1PDN6MEW=
ECC1 Mn23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DE[WlEPTB;Nj63OEDDuSByLkW5JO69VQ>? MlvJNlM1PDN6MEW=
HEC1B MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzVRnI4UUN3ME22MlQ2KMLzIECuOlch|ryP NXj0e5BtOjN2NEO4NFU>
USPC1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTVwN{WgxtEhOC53MDFOwG0> MoXiNlM1PDN6MEW=
SPAC1L MoqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnMWlBDUUN3ME20MlkzKMLzIECuOVAh|ryP MVyyN|Q1OzhyNR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pFGFR1 / FGFR1 / pFRS2 / FRS2 / MEK / ERK; 

PubMed: 28255027     


Immunoblot demonstrates the expression of total/pFGFRs and total/pFRS2 in DMSO and BGJ398 in treated cell lines A. DMS114. B. RT112. Lysates were prepared from cells exposed to BGJ398 (at the indicated concentrations) for 24h and immunoblots performed with the respective antibodies. Representative data are shown from three experimental replicates. Bar graphs display densitometric analysis of protein bands using GAPDH as control. BGJ398 treatment results in decreased levels of pFGFR1/pFGFR3 and pFRS2/total FRS2, respectively.

p-YAP (S127) / YAP; 

PubMed: 26826125     


Immunoblot analysis of serine 127-phosphorylated YAP (p-YAPS127) and total YAP in KMCH and KMBC cells treated with vehicle (Veh) or BGJ398 (10 μm) for 24 h. β-Actin was used as a loading control.

Mcl-1; 

PubMed: 26826125     


Immunoblot analysis (E) of Mcl-1 in KMCH and KMBC cells treated with vehicle or BGJ398 (10 μm) at several time points. β-Actin was used as a loading control.

Cyclin D1 / Cyclin A / Cyclin B / γ-H2AX / Cleaved caspase-9 / PARP ; 

PubMed: 30326563     


Cells were treated with indicated concentration of PTX and BGJ398 for 24 h. Expression of cyclin D1, cyclin A, cyclin B, γ-H2AX, caspase-9, PARP, and β-actin (loading control) was analyzed by Western blotting.

Snail / Slug / ZEB1; 

PubMed: 30326563     


PTX and BGJ398 combination treatment synergistically decreases the protein levels of EMT inducers Snail, Slug, and ZEB1.

p-FRS2 / FRS2 / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29654068     


Protein lysates from NCI-H2077 cells after treatment with DMSO or BGJ398 1 μM probed at different time points for key members of the canonical FGFR signaling pathway.

28255027 26826125 30326563 29654068
Immunofluorescence
YAP; 

PubMed: 26826125     


Immunofluorescence images (top panel) and percentage of YAP-positive nuclei (bottom panel) in KMCH and KMBC cells 24 h of treatment with 10 μmBGJ398. Mean ± S.E. are depicted for n = 3. **, p < 0.01. Scale bars: 50 μm.

26826125
Growth inhibition assay
Cell viability; 

PubMed: 28255027     


Resistance was induced by chronic exposure of DMS114, and RT112 cell lines to BGJ398. Control cells were treated with DMSO. Panel shows viability curves performed with CellTiter-Glo assay. Control and resistant cells were treated with BGJ398 at different concentrations as indicated, and viable cells were measured after 72h. The percentage of viable cells is shown relative to DMSO vehicle treated controls (mean ± SD). Assays were performed in quadruplicates (three experimental replicates).

IC50; 

PubMed: 30326563     


T24, J82, RT4, and UMUC-14 cells were treated with 0, 0.1, 1, and 10 μM BJG398 for 3 days. IC50 values were calculated using CalcuSyn (BioSoft, Ferguson, MO, USA). Data represent mean ± standard deviation of five replicates.

28255027 30326563
In vivo In this orthotopic xenograft bladder cancer model, BGJ398 induces tumor growth inhibition and stasis after oral administration for 12 consecutive days at the doses of 10 and 30 mg/kg, respectively. Interestingly, the animals that received BGJ398 exhibits either no body weight loss (10 mg/kg) or 10% body weight gain (30 mg/kg), a further indication of efficacy. RT112 tumor-bearing and female Rowett rats receive a single oral administration of the monophosphate salt of BGJ398 at the doses of 4.25 and 8.51 mg/kg. BGJ398 significantly decreases the levels of pFRS2 and pMAPK in a dose-dependent manner. BGJ398 inhibits significantly bFGF-stimulated angiogenesis in a dose-dependent manner. However, BGJ398 does not impair VEGF-induced blood vessel formation. [1]

Protocol

Kinase Assay: [1]
+ Expand

Radiometric kinase assay:

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 BGJ398 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 minutes in a final volume of 30 μL including BGJ398. 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 minutes 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 ished 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 the BGJ398.
Cell Research:[1]
+ Expand
  • Cell lines: Murine BaF3 cell lines
  • Concentrations: 0 μM-0.1 μM
  • Incubation Time: 48 hours
  • Method: Murine BaF3 cell lines, whose proliferation and survival has been rendered IL-3-independent by stable transduction with tyrosine kinases activated either by mutation or fusion with a dimerizing partner, 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. BGJ398-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. BGJ398 is serially diluted in DMSO and arrayed in a polypropylene 384-well plate. Then 50 nL of BGJ398 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 hours. 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 BGJ398 needed to reduce cell viability to 50% of a DMSO control.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Athymic nude-nu mice bearing parental RT112 cell line
  • Formulation: PEG300/D5W (2:1, v/v)
  • Dosages: 10 mg/kg/qd and 30 mg/kg/qd
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL warmed (1.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1%CMC-Na
For best results, use promptly after mixing.
30mg/mL

* 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.

Chemical Information

Molecular Weight 560.48
Formula

C26H31Cl2N7O3

CAS No. 872511-34-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03773302 Recruiting Advanced Cholangiocarcinoma|FGFR2 Gene Mutation QED Therapeutics Inc. March 2019 Phase 3
NCT03773302 Recruiting Advanced Cholangiocarcinoma|FGFR2 Gene Mutation QED Therapeutics Inc. March 2019 Phase 3
NCT03510455 Recruiting Tumor-Induced Osteomalacia National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC) February 27 2019 Phase 2
NCT03510455 Recruiting Tumor-Induced Osteomalacia National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC) February 27 2019 Phase 2
NCT02706691 Recruiting FGFR Gene Amplification|FGFR1 Gene Amplification|FGFR2 Gene Amplification|FGFR2 Gene Mutation|FGFR3 Gene Mutation|Head and Neck Squamous Cell Carcinoma|Human Papillomavirus Infection|Recurrent Head and Neck Carcinoma|Recurrent Nasopharynx Carcinoma|Recurrent Oropharyngeal Squamous Cell Carcinoma University of Chicago|Novartis June 1 2018 Phase 2
NCT02706691 Recruiting FGFR Gene Amplification|FGFR1 Gene Amplification|FGFR2 Gene Amplification|FGFR2 Gene Mutation|FGFR3 Gene Mutation|Head and Neck Squamous Cell Carcinoma|Human Papillomavirus Infection|Recurrent Head and Neck Carcinoma|Recurrent Nasopharynx Carcinoma|Recurrent Oropharyngeal Squamous Cell Carcinoma University of Chicago|Novartis June 1 2018 Phase 2

Tech Support

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Frequently Asked Questions

  • Question 1:

    If you have any suggestions about the formulation of this compound for a direct oral gavage administration?

  • Answer:

    BGJ398 (S2183) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30 mg/ml as a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID