BGJ398
(Synonyms: FGFR抑制剂(NVP-BGJ398),BGJ398,BGJ-398,Infigratinib) 目录号 : GC10055
An FGFR inhibitor
Cas No.:872511-34-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
|
Cell lines |
AN3CA, MFE296, MFE280, SNGM and HEC1A cells |
|
Preparation method |
The solubility of this compound in DMSO is |
|
Reaction Conditions |
0.5 μM, 72 hours |
|
Applications |
Exposure of AN3CA, MFE296, and MFE280 cells to the inhibitor led to a significant increase in the fraction of cells in G0–G1 arrest and to a significant increase in the fraction of cells undergoing apoptosis, when compared with untreated controls. In contrast, NVP-BGJ398 treatment did not alter the fractions of cells in G0–G1 arrest in the FGFR2 wild-type endometrial cancer cell lines SNGM or HEC1A in vitro. Moreover, NVP-BGJ398 treatment had no effect on apoptosis in the FGFR2 wild-type endometrial cancer cell line HEC1A. |
| Animal experiment: [1] | |
|
Animal models |
Nude mice bearing AN3CA, MFE296, SNGM or HEC1A xenografts |
|
Dosage form |
Oral administration, 30 or 50 mg/kg, daily |
|
Applications |
NVP-BGJ398 significantly delayed the growth of FGFR2-mutated endometrial cancer xenograft tumors. In contrast, NVP-BGJ398 had no in vivo inhibitory effects in the long-term study using the FGFR2 wild-type endometrial cancer cell line SNGM, but surprisingly did show in vivo activity in HEC1A cells by delaying tumor growth in these cells. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
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. |
|
NVP-BGJ398 is a potent, selective, and orally bioavailable inhibitor of the FGFR tyrosine kinases. NVP-BGJ398 is a small molecular with the formula of C26H31Cl2N7O3 and Molecular Weight of 560. The fibroblast growth factor receptor 1 (FGFR1), FGFR2, FGFR3, and FGFR4, encompasses the receptors for 18 different FGF ligands. These ligand–receptor combinations regulate a broad spectrum of signaling during development and in normal growth control. BGJ398 inhibits the cell proliferation and induces apoptosis in cancer cells and suppresses tumor growth in xenograft model.
References:
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
| Cas No. | 872511-34-7 | SDF | |
| 别名 | FGFR抑制剂(NVP-BGJ398),BGJ398,BGJ-398,Infigratinib | ||
| 化学名 | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea | ||
| 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 | ||
| 分子式 | C26H31Cl2N7O3 | 分子量 | 560.48 |
| 溶解度 | ≥ 7mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7842 mL | 8.9209 mL | 17.8418 mL |
| 5 mM | 0.3568 mL | 1.7842 mL | 3.5684 mL |
| 10 mM | 0.1784 mL | 0.8921 mL | 1.7842 mL |
| 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 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Abstract
NVP-BGJ398, a selective FGFR inhibitor, is capable of inhibiting FGFR2 signaling, inducing cell-cycle arrest and increasing apoptosis in FGFR2-mutant endometrial cancer cells, which exhibits inhibition against cell growth both in vivo and in vitro.
Abstract
Genetic alterations in FGFR family members are potential predictors of NVP-BGJ398 sensitivity, including FGFR1 amplication in osteosarcoma and FGF19 copy number gain at the 11q13 amplicon.
Abstract
NVP-BGJ398 exhibited potent antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3.