BGJ398 (NVP-BGJ398)

For research use only. Not for use in humans.

目录号:S2183 别名: Infigratinib

BGJ398 (NVP-BGJ398) Chemical Structure

Molecular Weight(MW): 560.48

BGJ398 (NVP-BGJ398)是一种有效的,选择性FGFR抑制剂,作用于FGFR1/2/3,在无细胞试验中IC50为0.9 nM/1.4 nM/1 nM,作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上,对Abl, Fyn, Kit, Lck, Lyn和Yes几乎没有抑制活性。Phase 2。

规格 价格 库存 购买数量  
RMB 902.78 现货
RMB 1411.94 现货
RMB 2215.49 现货
RMB 4650.25 现货
RMB 7960.75 现货
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客户使用Selleck生产的BGJ398 (NVP-BGJ398)发表文献138篇:

产品安全说明书

FGFR抑制剂选择性比较

生物活性

产品描述 BGJ398 (NVP-BGJ398)是一种有效的,选择性FGFR抑制剂,作用于FGFR1/2/3,在无细胞试验中IC50为0.9 nM/1.4 nM/1 nM,作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上,对Abl, Fyn, Kit, Lck, Lyn和Yes几乎没有抑制活性。Phase 2。
靶点
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
体外研究

BGJ398抑制FGFR3-K650E,IC50 为4.9 nM。此外, BGJ398 也抑制VEGFR2。BGJ398 抑制其他激酶,包括ABL, FYN, KIT, LCK, LYN 和 YES,IC50分别为2.3 μM, 1.9 μM, 0.75 μM, 2.5 μM, 0.3 μM和1.1 μM。在细胞水平, BGJ398 抑制FGFR1-, FGFR2-Q, 和FGFR3-依赖的BaF3 细胞增殖,IC50分别为2.9 μM, 2.0μM和2 μM。BGJ398在特定酪氨酸残基,包括FGFR-WT, FGFR2-WT, FGFR3-K650E, FGFR3-S249C 和 FGFR4-WT处,干扰自磷酸化,IC50分别为4.6 nM, 4.9 nM, 5 nM, 5 nM 和168 nM。BGJ398 抑制过量表达野生型(WT)FGFR3的癌细胞,如RT112, RT4, SW780 和JMSU1 的增殖,IC50分别为5 nM, 30 nM, 32 nM 和15 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC MmHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGxMVI2ODBibl2= MYi0PEBp MnP6xsBKSzVyPTCyN|U66oDLbn2= MY[yOVY5QDd2Mx?=
HCC NXTlT2dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGxMVI2ODBibl2= M{\idFQ5KGh? M{HyeWlEPTB;MUGyOQKBkW6v MYmyOVY5QDd2Mx?=
HCT116 NYTX[WRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[0PEBp NIH4d5lKSzVyPUOg{txO MYeyOFUxOzV|OB?=
HKH2 Mn3jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O5cFQ5KGh? MnPzTWM2OD12IN88US=> NWTWNVRsOjR3MEO1N|g>
RKO NWPHU24xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDI[4Q1QCCq M1zIOGlEPTB;MT6yJO69VQ>? M2fWT|I1PTB|NUO4
LS174T NUTVVmxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWO0PEBp MV\JR|UxRTRizszN M3zI[FI1PTB|NUO4
HCD9 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3FfmYxNjVvNTFOwG0> M1jhV|Q5Nzd{IHi= M1fs[GROW09? MnGx[IVkemWjc3XzJINmdGxidnnhZoltcXS7 MmfsNlQyOzV6MU[=
HCT116 NWC3TZBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi3eWFUOC53LUWg{txO M4jKXlQ5Nzd{IHi= NEm4U4RFVVOR NEPkc45l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NEXaTogzPDF|NUixOi=>
SNU-C1 NYSwPGlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn3NE42NTVizszN MmK1OFgwPzJiaB?= MYrEUXNQ NHzmWGxvdyCnZn\lZ5Q> M2jwNVI1OTN3OEG2
MFE280 M37CcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJwNkOgxtEhOC56MjFOwG0> NXXtT2tHOjN2NEO4NFU>
AN3CA NF3JVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwMECgxtEhOC5{MDFOwG0> NUOyd21IOjN2NEO4NFU>
HEC155 MoDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXvPGZUUUN3ME20Mlc1KMLzIEGuNFkh|ryP NHvRPZozOzR2M{iwOS=>
MFE296 NEDvOHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHmdXRKSzVyPUKuPFYhyrFiMD6yNEDPxE1? M3\hfVI{PDR|OEC1
SPAC1S M1nTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\yTWM2OD1|LkG5JOKyKDBwOUOg{txO MYOyN|Q1OzhyNR?=
RL952 M4DId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjkTZRKSzVyPUOuOFEhyrFiMD6yN{DPxE1? MoDpNlM1PDN6MEW=
EN1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7RUpdKSzVyPUSuO|UhyrFiMD62NkDPxE1? NIj4S2IzOzR2M{iwOS=>
SNGII M{nwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTRwMkmgxtEhOC53ODFOwG0> MXyyN|Q1OzhyNR?=
ISHIKAWA NXHNNHlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHrR5hlUUN3ME21MlQ5KMLzIECuNFMh|ryP NWXWb3ZuOjN2NEO4NFU>
HEC1A MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPNc|dKSzVyPUGwMlAxKMLzIEGuNFAh|ryP Mnz5NlM1PDN6MEW=
KLE NIrl[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTNwMEOgxtEhOC5zMTFOwG0> MnraNlM1PDN6MEW=
SNGM NFjsfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTVwMECgxtEhOC52MTFOwG0> Ml3tNlM1PDN6MEW=
USPC2 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjqSGRKSzVyPUeuNFAhyrFiMD6yNUDPxE1? M3fH[FI{PDR|OEC1
EN Mn7yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2SwcmlEPTB;Nj6wN{DDuSByLkOxJO69VQ>? MoL2NlM1PDN6MEW=
MFE319 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3HcnNTUUN3ME21MlM4KMLzIECuNFMh|ryP NF7INIIzOzR2M{iwOS=>
EFE184 M3\IeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvwVI5KSzVyPUiuNFQhyrFiMD62PUDPxE1? NULrW5k{OjN2NEO4NFU>
ECC1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DjNGlEPTB;Nj63OEDDuSByLkW5JO69VQ>? MmW4NlM1PDN6MEW=
HEC1B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTQTWM2OD14LkS1JOKyKDBwNkeg{txO NIjGU3EzOzR2M{iwOS=>
USPC1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTVwN{WgxtEhOC53MDFOwG0> M2\P[VI{PDR|OEC1
SPAC1L Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LhVGlEPTB;ND65NkDDuSByLkWwJO69VQ>? NED5U20zOzR2M{iwOS=>

... 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
体内研究 BGJ398按10和30 mg/kg剂量, 分别处理原位移植膀胱癌模型,持续12天,则抑制肿瘤生长,和引起淤血。BGJ398按10 mg/kg剂量处理实验动物,体重没有改变,按30 mg/kg剂量处理,则体重增加10%。BGJ398磷酸盐按 4.25和8.51 mg/kg剂量口服处理给药携带RT112肿瘤的雌性Rowett大鼠。BGJ398显著降低 pFRS2 和pMAPK水平,这种作用存在剂量依赖性。BGJ398显著抑制bFGF刺激的血管生成,这种作用存在剂量依赖性。然而, BGJ398不损害VEGF诱导的血管形成。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

放射性激酶实验:

在有放射性标记ATP存在时,通过纯化的GST-融合FGFR3-K650E激酶域,测定合成底物的磷酸化,而测定激酶活性。通过混合10 μL 3倍浓度BGJ398 溶液和10 μL相应底物混合物 (肽底物, ATP 和 [γ33P]ATP)测定酶活性。在实验buffer中加入10 μL 3倍浓度酶溶液开始反应。实验组成的终浓度如下:10 ng 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 聚(EY) 4:1, 1% DMSO 及0.5 μM ATP (γ-[33P]-ATP 0.1 μCi)。包括BGJ398的终体积为30 μL的实验混合物根据过滤结合(FB)法在96孔板上室温下进行实验10分钟。加入20 μL 125 mM EDTA终止酶反应,按如下测定33P 渗透到肽底物的量: 30 μL 终止反应混合物转移到Immobilon-PVDF 膜上,之前用甲醇浸泡膜5分钟,用水冲洗,用0.5% H3PO4浸泡5分钟, 然后安装在真空歧管中。点样,连接真空,然后使用0.5% H3PO4 (200 μL)冲洗细胞。 移除膜,在摇床上使用1% H3PO4 处理四次,再使用乙醇处理一次。烘干膜,在膜上每孔覆盖 10 μL闪烁液。封闭实验板,在微板闪烁计数板上读数。通过线性回归分析 BGJ398抑制百分数,而计算IC50值。
细胞实验:[1]
- 合并
  • Cell lines: 鼠BaF3细胞系
  • Concentrations: 0 μM-0.1 μM
  • Incubation Time: 48小时
  • Method: Murine 鼠BaF3细胞系接种在含10% FBS, 4.5 g/L葡萄糖, 1.5 g/L碳酸氢钠, 和Pen/Strep的 RPMI-1640培养基上。每周细胞传代两次。使用荧光素酶生物发光法检测测定BGJ398调节的抑制BaF3细胞增殖和活性。BaF3或 BaF3 Tel-TK细胞按每孔4250个细胞接种到384孔板上,在新鲜培养基中使用μFill液体分配器每孔加50 μL。BGJ398 在DMSO中连续稀释,然后排列在384孔板中。使用pintool传输设备使50 nL BGJ398 转移到含细胞的实验板上,然后实验板在37oC(5% CO2) 下温育48小时。然后加入25 μL Bright-Glo,使用 Analyst-GT测定荧光。测定IC50值。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带亲本RT112细胞系的无胸腺裸鼠
  • Dosages: 10 mg/kg/qd和30 mg/kg/qd
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 1 mg/mL warmed (1.78 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1%CMC-Na
30mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 560.48
化学式

C26H31Cl2N7O3

CAS号 872511-34-7
储存条件 粉状
溶于溶剂
别名 Infigratinib

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

FGFR Inhibitors with Unique Features

相关FGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID