BGJ398 (NVP-BGJ398)

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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BGJ398 (NVP-BGJ398) 化学構造
分子量: 560.48





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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。
IC50 0.9 nM 1.4 nM 1 nM 60 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HCT116 MlfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rNcFQ5KGh? M4PROmlEPTB;MzFOwG0> MkjCNlQ2ODN3M{i=
HKH2 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XI[FQ5KGh? MVjJR|UxRTRizszN M330O|I1PTB|NUO4
RKO NFey[YtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILhR2E1QCCq NHXuR3hKSzVyPUGuNkDPxE1? MVqyOFUxOzV|OB?=
LS174T NH32UmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVq0PEBp NWnpem9zUUN3ME20JO69VQ>? MkXENlQ2ODN3M{i=
HCD9 NHi2[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTnN|V7OC53LUWg{txO NFvUOpA1QC95MjDo NEfU[Y1FVVOR NEnSO|dl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= MlTENlQyOzV6MU[=
HCT116 NXnocpVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMlUuPSEQvF2= MUG0PE84OiCq NInhco5FVVOR MWfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? NIXJSIYzPDF|NUixOi=>
SNU-C1 MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDsNE42NTVizszN MlPEOFgwPzJiaB?= M{Xze2ROW09? Mmfwco8h\W[oZXP0 MnznNlQyOzV6MU[=
MFE280 M1racmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\IeVFKSzVyPUKuOlMhyrFiMD64NkDPxE1? Mn73NlM1PDN6MEW=
AN3CA M{nwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUToVplGUUN3ME2xMlAxKMLzIECuNlAh|ryP MV6yN|Q1OzhyNR?=
HEC155 M4exWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;Pb4hMUUN3ME20Mlc1KMLzIEGuNFkh|ryP MormNlM1PDN6MEW=
SPAC1S M4LQT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rWWWlEPTB;Mz6xPUDDuSByLkmzJO69VQ>? MVWyN|Q1OzhyNR?=
RL952 MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\lTWM2OD1|LkSxJOKyKDBwMkOg{txO M1i1flI{PDR|OEC1
EN1 NEfoUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\HTWM2OD12Lke1JOKyKDBwNkKg{txO MkWxNlM1PDN6MEW=
ISHIKAWA NGDN[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i0b2lEPTB;NT60PEDDuSByLkCzJO69VQ>? M{Xo[|I{PDR|OEC1
KLE NV;ocopPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2zblZwUUN3ME2zMlA{KMLzIECuNVEh|ryP NVe5cGNuOjN2NEO4NFU>
USPC2 NYGySolsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLhTWM2OD15LkCwJOKyKDBwMkGg{txO MXmyN|Q1OzhyNR?=
EN NIX2[2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTZwMEOgxtEhOC5|MTFOwG0> NEnXSIQzOzR2M{iwOS=>
MFE319 M2PyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrNdVlKSzVyPUWuN|chyrFiMD6wN{DPxE1? MUmyN|Q1OzhyNR?=
EFE184 NUT6W|NrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[zb29KSzVyPUiuNFQhyrFiMD62PUDPxE1? NIrufWszOzR2M{iwOS=>
ECC1 M{f3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFT6T25KSzVyPU[uO|QhyrFiMD61PUDPxE1? M3zSdVI{PDR|OEC1
USPC1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mne4TWM2OD13Lke1JOKyKDBwNUCg{txO NGe0dZgzOzR2M{iwOS=>
SPAC1L M1\xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTRwOUKgxtEhOC53MDFOwG0> MV2yN|Q1OzhyNR?=

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験 BGJ398 is currently in a Phase I clinical trial in the treatment of the renal tumors.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

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.

動物実験: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download BGJ398 (NVP-BGJ398) SDF
分子量 560.48


CAS No. 872511-34-7
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 1 mg/mL warming (1.78 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-(4-(4-ethylpiperazin-1-yl)phenylamino)pyrimidin-4-yl)-1-methylurea

文献中の引用 (17)

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.



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID