Home Angiogenesis FGFR inhibitor BLU9931 For research use only.

BLU9931

BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.

BLU9931 Chemical Structure

BLU9931 Chemical Structure

CAS No. 1538604-68-0

Purity & Quality Control

BLU9931 Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-453 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant after 72 hrs by CCK8 assay, IC50=0.32μM. 28523108
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay, IC50=2.34μM. 28523108
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay, IC50=3.76μM. 28523108
sf9 Function assay 60 mins Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay, IC50=0.0094μM. ChEMBL
sf9 Function assay 60 mins Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay, IC50=0.011μM. ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.
Targets
FGFR4 [1]
(Cell-free assay)		 FGFR3 [1]
(Cell-free assay)
3 nM 150 nM
In vitro
In vitro In MDA-MB-453 cells, BLU9931 potently inhibits phosphorylation of FGFR4 signaling pathway. BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, such as Hep 3B, HUH-7, and JHH-7 cell lines, with EC50 of <1 μM. BLU9931 also inhibits proliferation in PDX-derived cell lines with an intact FGFR4 signaling pathway. [1]
Kinase Assay FGFR1-4 Biochemical Assays
FGFR kinase inhibition assays are performed at KM for ATP. Picomolar to low nanomolar concentrations of FGFR proteins are incubated in 1× Kinase Reaction Buffer (KRB) with 1 μM of CSKtide and 50 to 250 of μM ATP at 25°C for 90 minutes in the presence or absence of a dosed concentration series of inhibitor. All reactions are terminated by the addition of Stop buffer, and plates are read on a Caliper EZReader2. IC50 values are fit with a four-parameter log[Inhibitor] versus response model with floating Hill Slope.
Cell Research Cell lines Hep 3B, HUH-7, JHH-7, PLC/PRF/5, SK-HEP-1, SNU-182, SNU-387, SNU-398, SNU-423, SNU-449, SNU-878 cells
Concentrations ~10 μM
Incubation Time 72-120 hours
Method Established and PDX-derived HCC cell lines are seeded in 96-well plates in respective growth media, allowed to attach overnight, and treated with a dilution series of test compounds for two cell-doubling times. Cell viability is determined by CellTiter-Glo, and results represented as background-subtracted relative light units normalized to a DMSO-treated control. Relative EC50 values are determined at 50% inhibition between the top and bottom plateau of the dose–response curve.
In Vivo
In vivo In mice bearing the FGF19-amplified Hep 3B liver tumors, BLU9931 (300 mg/kg, p.o.) leads to tumor regression and prevents this weight loss induced by tumors. In mice bearing the FGF19-overexpressing PDX-derived LIXC012 xenografts, treatment with BLU9931 (300 mg/kg, p.o.) also leads to tumor regression. [1]
Animal Research Animal Models Mice bearing LIXC012 tumors
Dosages ~300 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 509.38 Formula

C26H22Cl2N4O3
CAS No. 1538604-68-0 SDF Download BLU9931 SDF
Smiles CC1=C(C(=CC=C1)NC(=O)C=C)NC2=NC=C3C=C(C=CC3=N2)C4=C(C(=CC(=C4Cl)OC)OC)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (196.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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