BLU9931

For research use only.

Catalog No.S7819

10 publications

BLU9931 Chemical Structure

CAS No. 1538604-68-0

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.

Selleck's BLU9931 has been cited by 10 publications

1 Customer Review

  • (E,G) Microscopic appearance of peritoneal dissemination of YTN16 (E) without BLU9931 and (G) with BLU9931 treatment for 3 weeks. (F,H) Microscopic features of s.c. tumor of YTN16 (F) without BLU9931 and (H) with BLU9931 treatment for 3 weeks. YTN16 tumor under treatment with BLU9931 does not form glandular structures.

    Cancer Science, 2018, doi:10.1111/cas.13569. BLU9931 purchased from Selleck.

Purity & Quality Control

Choose Selective FGFR Inhibitors

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 NHLnbY5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXnZPYlPPzJiaILz MlnERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDV|IHPlcIx{KGijcnLvdolv\yCIR1\SOEB[OzZ5QzDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVA:OC5|Mt88UU4> NID1ZXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWyN|ExQCd-Mki1NlMyODh:L3G+
MCF7 NXTkeWZUSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NY\6S|lNPzJiaILz M1vzcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDlfJBz\XO|aX7nJIxwfyCuZY\lcJMhd2ZiRlfGVlQh[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUC9Nk4{PM7:TT6= NH;5UlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWyN|ExQCd-Mki1NlMyODh:L3G+
MDA-MB-231 MmLORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NF\nNZA4OiCqcoO= NIrDd5dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiZYjwdoV{e2mwZzDsc5chdGW4ZXzzJI9nKE[JRmK0JIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyPUOuO|bPxE1w NGey[2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWyN|ExQCd-Mki1NlMyODh:L3G+
sf9 NVXtbHBMTnWwY4Tpc44h[XO|YYm= MWO2NEBucW6| M3nBd2lvcGmkaYTpc44hd2Zibn;uMZBpd3OyaH;yfYxifGWmIF6teIVzdWmwYXygTIl{Pi22YXfn[YQhTkeIUkSgR|Q4P0FibYX0ZY51KCiJNESyJJRwKEV5NUOgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKHOoOTDj[YxteyC3c3nu[{A2NU[udX:tRYh5NUuNS1vFSWl[Tk[IRz3OTFIh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIH3pcpMh[nlibXnjdo9ndHWrZHnjJI1w[mmuaYT5JJNpcW[2IHHzd4F6NCCLQ{WwQVAvODB7NN88UU4> MlPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFA3QDh7Nj:nQmNpTU2ETEyvZV4>
sf9 M3XHO2Z2dmO2aX;uJIF{e2G7 MlrUOlAhdWmwcx?= MoW5TY5pcWKrdHnvckBw\iC5aXzkJJR6eGVibn;uMZBpd3OyaH;yfYxifGWmIF6teIVzdWmwYXygTIl{Pi22YXfn[YQhTkeIUkSgLGc1PDJidH:gSVc2OyC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gd4Y6KGOnbHzzJJV{cW6pIEWtSox2dy2DaIitT2tMU0WHSWnGSmZINU6KMjDhd{B{fWK|dILheIUh[W[2ZYKgOlAhdWmwczDifUBucWO{b3\seYllcWNibX;ibYxqfHlic3jp[pQh[XO|YYmsJGlEPTB;MD6wNVHPxE1w NYS4THlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDB4OEi5Ok8oRkOqRV3CUFww[T5?

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
- Collapse

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]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Mice bearing LIXC012 tumors
  • Dosages: ~300 mg/kg
  • Administration: p.o.
    (Only for Reference)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 509.38
Formula

C26H22Cl2N4O3

CAS No. 1538604-68-0
Storage powder
in 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

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 ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

FGFR Signaling Pathway Map

Related FGFR Products

Tags: buy BLU9931 | BLU9931 supplier | purchase BLU9931 | BLU9931 cost | BLU9931 manufacturer | order BLU9931 | BLU9931 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID