BLU9931

Catalog No.S7819

For research use only.

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

CAS No. 1538604-68-0

Selleck's BLU9931 has been cited by 11 Publications

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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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-453 MlzFRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NH\nVnI4OiCqcoO= MkD2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDV|IHPlcIx{KGijcnLvdolv\yCIR1\SOEB[OzZ5QzDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVA:OC5|Mt88UU4> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV{M{GwPEc,Ojh3MkOxNFg9N2F-
MCF7 NUm2eFFCSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MYq3NkBpenN? MnfBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHX4dJJme3OrbnegcI94KGyndnXsd{Bw\iCIR1\SOEBi\nSncjC3NkBpenNiYomgR2NMQCCjc4PhfUwhUUN3ME2yMlM1|ryPLh?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV{M{GwPEc,Ojh3MkOxNFg9N2F-
MDA-MB-231 M3fRN2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MV:3NkBpenN? NIfGVVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiZYjwdoV{e2mwZzDsc5chdGW4ZXzzJI9nKE[JRmK0JIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyPUOuO|bPxE1w NWXxZXhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1NlMyODhpPkK4OVI{OTB6PD;hQi=>
sf9 NWTQTmR[TnWwY4Tpc44h[XO|YYm= M4PiSlYxKG2rboO= NGLo[3BKdmirYnn0bY9vKG:oIH7vck1xcG:|cHjvdplt[XSnZDDOMZRmem2rbnHsJGhqezZvdHHn[4VlKE[JRmK0JGM1PzeDIH31eIFvfCBqR{S0NkB1dyCHN{WzJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiC|ZkmgZ4VtdHNidYPpcochPS2IbIXvMWFpgC2NS1vLSWVKYU[IRletUmgzKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IH3pZ5Jw\my3aXTpZ{Bud2KrbHn0fUB{cGmodDDhd5NigSxiSVO1NF0xNjByOUVOwG0v M{H0XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQxPjh6OU[vK|5EcEWPQly8M4E,
sf9 MX7GeY5kfGmxbjDhd5NigQ>? M2DB[VYxKG2rboO= MXjJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCwb36tdIhwe3Cqb4L5cIF1\WRiTj30[ZJucW6jbDDIbZM3NXSjZ3fl[EBHT0[UNDCoS|Q1OiC2bzDFO|U{KHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDz[lkh[2WubIOgeZNqdmdiNT3GcJVwNUGqeD3LT2tMTUWLWV\GSmcuVkh{IHHzJJN2[nO2cnH0[UBi\nSncjC2NEBucW6|IHL5JI1q[3KxZnz1bYRq[yCvb3LpcIl1gSC|aHnmeEBie3OjeTygTWM2OD1yLkCxNe69VS5? MnW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFA3QDh7Nj:nQmNpTU2ETEyvZV4>
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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:[1]
  • 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.
Animal Research:[1]
  • Animal Models: Mice bearing LIXC012 tumors
  • Dosages: ~300 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 4 mg/mL warmed
(7.85 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% carboxymethylcellulose+1% Tween 80 as a suspension
For best results, use promptly after mixing.

30mg/mL

Chemical Information

Molecular Weight 509.38
Formula

C26H22Cl2N4O3

CAS No. 1538604-68-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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