BGJ398
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NVP-BGJ398是一种有效的、选择性的和可口服的FGFR酪氨酸激酶小分子抑制剂,分子式为C26H31Cl2N7O3,分子量为560。成纤维细胞生长因子受体1(FGFR1)、FGFR2、FGFR3和FGFR4是18种不同FGF配体的受体。这些配体-受体共同调节发育和正常生长控制期间的各种信号。BGJ398抑制癌细胞中细胞增殖,诱导细胞凋亡,并抑制异种移植模型中肿瘤的生长。
参考文献:
1. Fibroblast Growth Factor Receptors as Novel Therapeutic Targets in SNF5-Deleted Malignant Rhabdoid Tumors. S Wöhrle, A Weiss, M Ito, A Kauffmann, M Murakami. PLOS ONE. 2013
2. Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth. F Harbinski, VJ Craig, S Sanghavi, D Jeffery, L Liu. Cancer Discovery, 2012
- 1. Longwei Hu, Yang Wang, et al. "Apoptosis repressor with caspase recruitment domain (ARC) promotes bone regeneration of bone marrow-derived mesenchymal stem cells by activating Fgf-2/PI3K/Akt signaling." Stem Cell Res Ther. 2021 Mar 16;12(1):185. PMID:33726822
- 2. Day EK, Sosale NG, et al. "Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling." Cell Rep. 2020;30(10):3383-3396.e7. PMID:32160544
- 3. Serra M, Alysandratos KD, et al."Pluripotent stem cell differentiation reveals distinct developmental pathways regulating lung- versus thyroid-lineage specification." Development. 2017 Nov 1;144(21):3879-3893. PMID:28947536
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 560.48 |
Cas No. | 872511-34-7 |
Formula | C26H31Cl2N7O3 |
Synonyms | BGJ398,BGJ-398 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥7 mg/mL in DMSO with gentle warming |
Chemical Name | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea |
SDF | Download SDF |
Canonical SMILES | CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
AN3CA、MFE296、MFE280、SNGM和HEC1A细胞 |
溶解方法 |
该化合物在DMSO中的溶解度小于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
0.5 μM,72 hours |
实验结果 |
与未处理的对照相比,使用抑制剂处理的AN3CA、MFE296和MFE280细胞阻滞在G0-G1的细胞比例显著增加,并且经历凋亡的细胞比例也显著增加。相比之下,NVP-BGJ398处理未改变FGFR2野生型子宫内膜癌细胞系SNGM或HEC1A的G0-G1阻滞的细胞百分比。此外,NVP-BGJ398处理对FGFR2野生型子宫内膜癌细胞系HEC1A中的凋亡没有影响。 |
动物实验[1]: | |
动物模型 |
AN3CA、MFE296、SNGM或HEC1A异种移植裸鼠 |
剂量 |
口服,30或50 mg/kg,每天 |
实验结果 |
NVP-BGJ398显著延迟了FGFR2突变的子宫内膜癌异种移植肿瘤的生长。相比之下,在FGFR2野生型子宫内膜癌细胞系SNGM的长期研究中,没有发现NVP-BGJ398的体内抑制效应,令人惊讶的是,通过延迟这些细胞中的肿瘤生长,确实观察到了在HEC1A细胞中的体内活性。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Konecny G E, Kolarova T, O'Brien N A, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Molecular cancer therapeutics, 2013, 12(5): 632-642. |
描述 | BGJ398 (NVP-BGJ398)是一种有效的和选择性的FGFR抑制剂,作用于FGFR1/2/3,IC50值为0.9 nM/1.4 nM/1 nM,对FGFR的选择性比FGFR4和VEGFR2高40倍以上,对Abl、Fyn、Kit、Lck、Lyn和Yes几乎没有作用。 | |||||
靶点 | FGFR1 | FGFR2 | FGFR3 | FGFR4 | ||
IC50 | 0.9 nM | 1.4 nM | 1 nM | 60 nM |
质量控制和MSDS
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