BGJ398 (NVP-BGJ398)


BGJ398 (NVP-BGJ398)化学構造


BGJ398 (NVP-BGJ398)は一種の有効で、選択性的なFGFR阻害剤で、無細胞試験でFGFR1/2/3に作用する時のIC50値が0.9 nM/1.4 nM/1 nMです。BGJ398 (NVP-BGJ398)は、FGFRに作用する選択性はFGFR4とVEGFR2に作用する選択性より40倍以上が高くなリますが、Abl、Fyn、Kit、Lck、LynとYesを抑制する活性が殆どありません。臨床2期。

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  • Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIN3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 µM BGJ398, and 0.2 and 1 µM PD173074 were immunoblotted with the relevant antibodies. β-actin was used as a loading control.

    Hepatology 2014 59(4), 1427-34. BGJ398 (NVP-BGJ398) purchased from Selleck.

    Anchorage-independent growth of NIN3T3 cells expressing FGFR2 fusions and its suppression by FGFR inhibitors (BGJ: BGJ398 and PD: PD173074). The percentage (+/- s.d.) of colonies formed in the presence of FGFR2 inhibitors (0.2 礛) and by KD mutants with respect to those formed by DMSO-treated cells are plotted at the bottom. The NIH3T3 clone expressing EZR-ROS1 was used as a negative control for FGFR inhibitors. *P<0.05.

    Hepatology 2014 59(4), 1427-34. BGJ398 (NVP-BGJ398) purchased from Selleck.

  • we used a FGFR inhibitor (BGJ398) and a MEK inhibitor (PD98059) to confirm that the inhibition of FGF pathway was directly related to the fibroblast-like conversion, and same morphologic change and increased expression of Vim and COL I was observed

    Oncogene, 2017.. BGJ398 (NVP-BGJ398) purchased from Selleck.

    BGJ398 inhibits signaling in cell lines with activating FGFR alterations. 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 24 hours 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 a control. BGJ398 treatment results in decreased levels of pFGFR1/pFGFR3 and pFRS2/total FRS2, respectively.

    Mol Cancer Ther, 2017.. BGJ398 (NVP-BGJ398) purchased from Selleck.

  • BGJ39 distinctly inhibited the inductive effect of FGF2. Just as the results of western blot, BGJ39 not only reversed the down-expression of E-cadherin, but also weakened the expression of BSP and OPN. However, combination of both TGF- β1 and FGF2 containing BGJ39 distinctly improved the expression of fibronectin and periostin. β-actin was used as an internal control for equal protein loading. * P < 0.05, ** P < 0.01.

    J Cell Physiol 2014 229(11), 1647-59. BGJ398 (NVP-BGJ398) purchased from Selleck.




製品説明 BGJ398 (NVP-BGJ398)は一種の有効で、選択性的なFGFR阻害剤で、無細胞試験でFGFR1/2/3に作用する時のIC50値が0.9 nM/1.4 nM/1 nMです。BGJ398 (NVP-BGJ398)は、FGFRに作用する選択性はFGFR4とVEGFR2に作用する選択性より40倍以上が高くなリますが、Abl、Fyn、Kit、Lck、LynとYesを抑制する活性が殆どありません。臨床2期。
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

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC NYjuNIFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxMVI2ODBibl2= MVy0PEBp NVzWN2MzyqCLQ{WwQUAzOzV74pEJco0> NXy0W4dWOjV4OEi3OFM>
HCC NG[xVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPrNU0zPTByIH7N MV20PEBp MlP0TWM2OD1zMUK05qCKdm1? NGC5ZWQzPTZ6OEe0Ny=>
HCT116 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPqblcxPDhiaB?= MkHOTWM2OD1|IN88US=> NG\qTFQzPDVyM{WzPC=>
HKH2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnpOFghcA>? NET4UGFKSzVyPUSg{txO MVWyOFUxOzV|OB?=
RKO M3[0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWG0PEBp MVTJR|UxRTFwMjFOwG0> MXSyOFUxOzV|OB?=
LS174T MnfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fUPFQ5KGh? MVXJR|UxRTRizszN M3nQNlI1PTB|NUO4
HCD9 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXyW5AxNjVvNTFOwG0> MYi0PE84OiCq MlLRSG1UVw>? M3HiUoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= NIm2NGczPDF|NUixOi=>
SNU-C1 M1Xvb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvuNE42NTVizszN NHrLWpE1QC95MjDo M2\RemROW09? Mn;qco8h\W[oZXP0 NI\SNY4zPDF|NUixOi=>
MFE280 NIHxdVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHsWGlKSzVyPUKuOlMhyrFiMD64NkDPxE1? M2HUeFI{PDR|OEC1
HEC155 M1:1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\jOIJwUUN3ME20Mlc1KMLzIEGuNFkh|ryP MnG3NlM1PDN6MEW=
MFE296 NEjZN2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzYNoxIUUN3ME2yMlg3KMLzIECuNlAh|ryP MkLMNlM1PDN6MEW=
RL952 Ml\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC0eFJyUUN3ME2zMlQyKMLzIECuNlMh|ryP MX:yN|Q1OzhyNR?=
EN1 NH3FV3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHCcVRKSzVyPUSuO|UhyrFiMD62NkDPxE1? MWiyN|Q1OzhyNR?=
SNGII Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTRwMkmgxtEhOC53ODFOwG0> MkDINlM1PDN6MEW=
KLE NH;XU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIn1bI1KSzVyPUOuNFMhyrFiMD6xNUDPxE1? MUKyN|Q1OzhyNR?=
SNGM Mo\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTVwMECgxtEhOC52MTFOwG0> NHrUUokzOzR2M{iwOS=>
EN M1T5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTZwMEOgxtEhOC5|MTFOwG0> NVfMZZpYOjN2NEO4NFU>
MFE319 M2mxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\kcGlEPTB;NT6zO{DDuSByLkCzJO69VQ>? M2O3[FI{PDR|OEC1
EFE184 NU[2flYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:wV2lEPTB;OD6wOEDDuSByLk[5JO69VQ>? NFHhSWkzOzR2M{iwOS=>
ECC1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnyW3NKSzVyPU[uO|QhyrFiMD61PUDPxE1? NHX4cJIzOzR2M{iwOS=>
HEC1B MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz2[XdKSzVyPU[uOFUhyrFiMD62O{DPxE1? MmfrNlM1PDN6MEW=


体内試験 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]


キナーゼ試験: [1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: Murine BaF3 cell lines
  • 濃度: 0 μM-0.1 μM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
+ 展開
  • 動物モデル: Athymic nude-nu mice bearing parental RT112 cell line
  • 製剤: PEG300/D5W (2:1, v/v)
  • 投薬量: 10 mg/kg/qd and 30 mg/kg/qd
  • 投与方法: Oral administration

溶解度 (25°C)

体外 DMSO 1 mg/mL (1.78 mM) warming
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 560.48


CAS No. 872511-34-7
in solvent
別名 N/A





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • 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):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02706691 Not yet recruiting Head and Neck Squamous Cell Carcinoma University of Chicago October 2016 Phase 2
NCT02657486 Recruiting Bladder Cancer|Non-Muscle-Invasive Urothelial Carcinoma Memorial Sloan Kettering Cancer Center January 2016 --
NCT02312804 Withdrawn Cancer of Cervix|Tumors The University of Texas Health Science Center at San Antonio January 2015 Phase 1
NCT02257541 Recruiting Advanced Gastrointestinal Stromal Tumor (GIST) Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|M.D. Anderson Cancer Center|University of Pittsburgh October 2014 Phase 1|Phase 2
NCT02160041 Recruiting Solid Tumor|Hematologic Malignancies Novartis Pharmaceuticals|Novartis July 2014 Phase 2
NCT02150967 Active, not recruiting Advanced Cholangiocarcinoma Novartis Pharmaceuticals|Novartis July 2014 Phase 2



Handling Instructions


  • * 必須


  • 問題1:

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

  • 回答:

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


FGFR Inhibitors with Unique Features


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID