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Infigratinib

产品编号 T1975 CAS 872511-34-7

别名: BGJ-398, NVP-BGJ398

Infigratinib (NVP-BGJ398) 是一种 FGFR 家族抑制剂，抑制 FGFR1，FGFR2，FGFR3和 FGFR4的 IC50分别为 0.9 nM，1.4 nM，1 nM，60 nM。

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Infigratinib, CAS 872511-34-7

规格	价格/CNY	货期
1 mg	￥ 185	现货
5 mg	￥ 413	现货
10 mg	￥ 497	现货
25 mg	￥ 736	现货
50 mg	￥ 997	现货
100 mg	￥ 1,620	现货
200 mg	￥ 2,660	现货
500 mg	￥ 5,460	现货
1 mL * 10 mM (in DMSO)	￥ 455	现货

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其他形式的 Infigratinib:

选择批次

纯度: 98.46%

纯度: 98.03%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Infigratinib (NVP-BGJ398) (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC50: 0.9/1.4/1 nM for FGFR1/2/3), >40-fold selective for FGFR versus FGFR4 and VEGFR2.
靶点活性	FGFR4:60 nM (cell free), FGFR3:1.0 nM (cell free), FGFR3 (K650E):4.9 nM (cell free), FGFR1:0.2 nM (cell free), FGFR2:1.4 nM (cell free)
体外活性	Infigratinib (NVP-BGJ398) inhibited FGFR1/2/3 (IC50: 1 nM), FGFR3-K650E (IC50: 4.9 nM), and FGFR4 (IC50: 60 nM). NVP-BGJ398 inhibited the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values which were in the low nanomolar range and comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay [1]. Among the 35 cell lines selected from the high-throughput assays, 28 were confirmed as sensitive to NVP-BGJ398 (IC50s: 0.001 to 500 nmol/L). Collectively, among the 541 (517 + 24) cell lines from the CCLE subjected to viability testing, 5.9% were found to be sensitive to NVP-BGJ398 [2]. Cell lines with activating FGFR2 mutations (S252W, N550K) were more sensitive to NVP-BGJ398 when compared with their FGFR2 wild-type counterparts. NVP-BGJ398 was potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells [3].
体内活性	When tested in this orthotopic xenograft bladder cancer model, NVP-BGJ398 (10 and 30 mg/kg) induced tumor growth inhibition and stasis after oral administration for 12 consecutive days. The monophosphate salt of 1h was orally administered to juvenile, immunocompromised, female Rowett rats for 20 consecutive days (20 administrations) at the doses of 5, 10, and 15 mg/kg/qd (free base equivalents). Nearly complete tumor stasis was achieved at the lowest dose while no overt toxicity was observed. The doses of 10 and 15 mg/kg provided tumor regression which was accompanied by a dose-dependent decrease of body weight [1]. NVP-BGJ398 (30 mg/kg, p.o.) significantly delayed the growth of FGFR2-mutated endometrial cancer xenograft tumors. NVP-BGJ398 had no in vivo inhibitory effects in the long-term study using the FGFR2 wild-type endometrial cancer cell line SNGM [2].
激酶实验	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 NVP-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 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 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].
细胞实验	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, were cultured in RPMI-1640 media supplemented with 10% FBS, 4.5 g/L glucose, 1.5 g/L sodium bicarbonate, and Pen/Strep. Cells were passaged twice weekly. Compound-mediated inhibition of BaF3 cell proliferation and viability was assessed using a Luciferase bioluminescent assay. Exponentially growing BaF3 or BaF3 Tel-TK cells were seeded into 384-well plates (4250 cells/well) at 50 μL/well using a μFill liquid dispenser in fresh medium. NVP-BGJ398 was serially diluted in DMSO and arrayed in a polypropylene 384-well plate. Then 50 nL of compound was transferred into the plates containing the cells by using the pintool transfer device, and the plates incubated at 37 ℃ (5% CO2) for 48 h. Then 25 μL of Bright-Glo were added, and luminescence was quantified using an Analyst-GT. Custom curve-fitting software was used to produce a logistic fit of percent cell viability as a function of the logarithm of inhibitor concentration. The IC50 value was determined as the concentration of compound needed to reduce cell viability to 50% of a DMSO control [1].
动物实验	We used FGFR2-mutated MFE296, AN3CA, and FGFR2 wild-type SNGM and HEC1A endometrial cancer cells, which spontaneously formed xenografts in athymic mice for our in vivo studies. Mice were maintained and handled under aseptic conditions, and animals were allowed access to food and water ad libitum. Female athymic mice (20.0–30.0 g) aged 4 to 6 weeks from an outbred strain (CD1 nu/nu) were injected subcutaneously (2 × 10^7 cells per mouse) in the flank. AN3CA cells were suspended in Matrigel and DMEM (volume 1:1). A period of 7 days elapsed to allow the formation of tumor nodules (mean xenograft volume = 105 ± 5.6 mm^3). Mice were then stratified into treatment groups with one tumor per mouse on the basis of their weight and tumor volume at the start of the experiment, such that the starting weight and tumor volume in each group were uniform. Mice (10/group) were treated via oral gavage of (i) vehicle control (5 mmol/L sodium citrate and 1 μL 6N HCL/mL), (ii) NVP-BGJ398 30 mg/kg (6 mg in 0.5 mL PEG300 and 0.5 mL acetic acid/acetate buffer, pH 4.68), (iii) dovitinib 30 mg/kg (1 mg in 1 mL of 5 mmol/L sodium citrate and 1 μL 6N HCL/mL), and (iv) dovitinib 50 mg/kg (1 mg in 1 mL of 5 mmol/L sodium citrate and 1 μL 6N HCL/mL). Treatment was continuous on a daily basis. Tumors were monitored by serial micrometer measurements made by a single observer with tumor volumes calculated length × width × depth. Differences in xenograft volume between groups were analyzed by Student t test of the tumor volume data [3].

别名	BGJ-398, NVP-BGJ398
分子量	560.48
分子式	C26H31Cl2N7O3
CAS No.	872511-34-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.61 mg/mL (10 mM), Sonification is recommended

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7842 mL	8.9209 mL	17.8418 mL	44.6046 mL
	5 mM	0.3568 mL	1.7842 mL	3.5684 mL	8.9209 mL
	10 mM	0.1784 mL	0.8921 mL	1.7842 mL	4.4605 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

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-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. 2. Guagnano V, et al. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov. 2012 Dec;2(12):1118-33. 3. 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. 4. Lin H, Lu P, Zhou M, et al. Purification of recombinant human fibroblast growth factor 13 in E. coli and its molecular mechanism of mitogenesis[J]. Applied microbiology and biotechnology. 2019: 1-11. 5. Pu X, Ye Q, Cai J, et al. Typing FGFR2 translocation determines the response to targeted therapy of intrahepatic cholangiocarcinomas[J]. Cell death & disease. 2021, 12(3): 1-14.

文献引用

1. Lidsky M E, Wang Z, Lu M, et al. Leveraging patient derived models of FGFR2 fusion positive intrahepatic cholangiocarcinoma to identify synergistic therapies. npj Precision Oncology. 2022, 6(1): 1-17. 2. Pu X, Ye Q, Cai J, et al. Typing FGFR2 translocation determines the response to targeted therapy of intrahepatic cholangiocarcinomas. Cell death & disease. 2021 Mar 11;12(3):256. doi: 10.1038/s41419-021-03548-4. 3. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866. 4. Lin H, Lu P, Zhou M, et al. Purification of recombinant human fibroblast growth factor 13 in E. coli and its molecular mechanism of mitogenesis. Applied Microbiology and Biotechnology. 2019: 1-11 5. Yang N, Fan Z, Sun S, et al.Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation.European Journal of Medicinal Chemistry.2023: 115857.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Infigratinib 872511-34-7 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR Fibroblast growth factor receptor BGJ 398 BGJ-398 NVP-BGJ398 inhibit Inhibitor NVP-BGJ-398 NVP-BGJ 398 BGJ398 inhibitor

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Infigratinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

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