Name: BLU9931
Brand: Selleck Chemicals
SKU: S7819
Rating: 5 (21 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl
Other FGFR Inhibitors	PD173074 AZD4547 (Fexagratinib) Futibatinib (TAS-120) LY2874455 PD-166866 Zoligratinib (Debio-1347) H3B-6527 Fisogatinib (BLU-554) SSR128129E Ferulic Acid

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	509.38	Formula	C₂₆H₂₂Cl₂N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1538604-68-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (196.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% carboxymethylcellulose 1 1% Tween 80 as a suspension Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (19.63mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% carboxymethylcellulose+1% Tween 80 clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	FGFR4 (Cell-free assay) 3 nM FGFR3 (Cell-free assay) 150 nM
In vitro	In MDA-MB-453 cells, BLU9931 potently inhibits phosphorylation of FGFR4 signalling pathway. This compound inhibits proliferation of HCC cell lines that express an intact FGFR4 signalling complex, such as Hep 3B, HUH-7, and JHH-7 cell lines, with EC50 of <1 μM. It also inhibits proliferation in PDX-derived cell lines with an intact FGFR4 signalling pathway.
Kinase Assay	FGFR1-4 Biochemical Assays
Kinase Assay	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 this compound. 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.
In vivo	In mice bearing the FGF19-amplified Hep 3B liver tumours, BLU9931 (300 mg/kg, p.o.) leads to tumour regression and prevents this weight loss induced by tumours. In mice bearing the FGF19-overexpressing PDX-derived LIXC012 xenografts, treatment with this compound also leads to tumour regression.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25776529/

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BLU9931 FGFR inhibitor

Chemical Structure

Molecular Weight: 509.38