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BGJ398

FGFR inhibitor

BGJ398

Catalog No. A3014
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
5mg $80.00 In stock
10mg $120.00 In stock
200mg $780.00 In stock

All inclusive: Shipping and all other fees included

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

BGJ398

Related Biological Data

BGJ398
Immunoblot analysis of p-FRS2 and p-ERK1/2 in MRT lines treated with DMSO or NVP-BGJ398 for 40 min as indicated. Total ERK1/2 and b-Tubulin expression was used to monitor equal loading.

Biological Activity

Description BGJ398 (NVP-BGJ398) is a potent and selective inhibitor of FGFR for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
Targets FGFR1 FGFR2 FGFR3 FGFR4    
IC50 0.9 nM 1.4 nM 1 nM 60 nM    

Protocol

Cell experiment: [1]

Cell lines

AN3CA, MFE296, MFE280, SNGM and HEC1A cells

Preparation method

Soluble in DMSO to 2 mg/ml. Stock solution can be stored at -80 °C less than 6 months.

Reacting condition

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

Application

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.

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Chemical Properties

Cas No. 872511-34-7 SDF Download SDF
Synonyms BGJ398,BGJ-398
Chemical Name 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
Formula C26H31Cl2N7O3 M.Wt 560.48
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

1. 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. doi: 10.1158/1535-7163.MCT-12-0999. Epub 2013 Feb 26.
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.
2. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov. 2012 Dec;2(12):1118-33. doi: 10.1158/2159-8290.CD-12-0210. Epub 2012 Sep 20.
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.

Background

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