BLU9931
Based on 10 publication(s) in Google Scholar
BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.97%
- CAS No.: 1538604-68-0
- Formule: C26H22Cl2N4O3
- Masse moléculaire:509.38
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) BLU9931
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]
- Int J Biol Sci. 2021 Jun 22;17(10):2576-2589. [Abstract]
- Clin Transl Med. 2022 Nov;12(11):e1102. [Abstract]
- Eur J Med Chem. 2023 Nov 5:259:115703. [Abstract]
- Commun Biol. 2025 Dec 15. [Abstract]
- Int J Oncol. 2017 Nov;51(5):1611-1620. [Abstract]
- J Biol Chem. 2022 Sep;298(9):102310. [Abstract]
- Clin Immunol. 2026 Apr:284:110664. [Abstract]
- University of Auckland. 2025.
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WB
Activité biologique
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FGFR1 591 nM (IC50) |
FGFR2 493 nM (IC50) |
FGFR3 150 nM (IC50) |
FGFR4 3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>5000 nM
Compound: BLU9931
|
Antiproliferative activity against mouse BaF3 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 38432058] |
| BaF3 | IC50 |
1.9 nM
Compound: BLU9931
|
Antiproliferative activity against mouse BaF3 cells expressing FGFR4 incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing FGFR4 incubated for 72 hrs by CCK-8 assay
|
[PMID: 38432058] |
| BaF3 | IC50 |
5.12 nM
Compound: BLU9931
|
Antiproliferative activity against mouse BaF3 transfected with FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 transfected with FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 37556948] |
| Epithelial cell | IC50 |
18.42 μM
Compound: BLU9931
|
Antiproliferative activity against human Intestinal epithelial cell assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human Intestinal epithelial cell assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 37556948] |
| HCT-116 | IC50 |
8.89 μM
Compound: BLU9931
|
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 37556948] |
| Hep 3B2 | EC50 |
62 nM
Compound: BLU9931; 2
|
Antiproliferative activity against human Hep3B cells measured after 4 days by Celltiter-glo based luminescent assay
Antiproliferative activity against human Hep3B cells measured after 4 days by Celltiter-glo based luminescent assay
|
[PMID: 38604131] |
| Hep 3B2 | IC50 |
0.058 μM
Compound: 1a; BLU9931
|
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
|
[PMID: 33859803] |
| Hep 3B2 | IC50 |
0.288 μM
Compound: BLU9931
|
Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by Cell Titer-Glo assay
Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by Cell Titer-Glo assay
|
[PMID: 33218898] |
| Hep 3B2 | IC50 |
550 nM
Compound: 5
|
Cytotoxicity against human Hep 3B2.1-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth
Cytotoxicity against human Hep 3B2.1-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth
|
[PMID: 35119278] |
| Hep 3B2 | IC50 |
72 nM
Compound: 15; BLU9931
|
Antiproliferative activity against human Hep3B cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human Hep3B cells incubated for 72 hrs by CCK8 assay
|
[PMID: 33030342] |
| HepG2 | IC50 |
5.458 μM
Compound: BLU9931
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 33618175] |
| Huh-7 | IC50 |
0.929 μM
Compound: BLU9931
|
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
|
[PMID: 34488024] |
| Huh-7 | IC50 |
191 nM
Compound: 5; BLU9931
|
Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay
Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay
|
[PMID: 38706130] |
| Huh-7 | IC50 |
327 nM
Compound: 2; BLU9931
|
Inhibition of cell proliferation in human Huh-7 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay
Inhibition of cell proliferation in human Huh-7 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay
|
[PMID: 35549181] |
| Huh-7 | IC50 |
5.386 μM
Compound: BLU9931
|
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 33618175] |
| Huh-7 | IC50 |
84 nM
Compound: 15; BLU9931
|
Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by CCK8 assay
|
[PMID: 33030342] |
| MCF7 | IC50 |
2.34 μM
Compound: 1; BLU9931
|
Antiproliferative activity against human MCF7 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay
|
[PMID: 28523108] |
| MDA-MB-231 | IC50 |
3.76 μM
Compound: 1; BLU9931
|
Antiproliferative activity against human MDA-MB-231 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay
|
[PMID: 28523108] |
| MDA-MB-435 | IC50 |
0.039 μM
Compound: 1a; BLU9931
|
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
|
[PMID: 33859803] |
| MDA-MB-453 | IC50 |
0.32 μM
Compound: 1; BLU9931
|
Antiproliferative activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant after 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant after 72 hrs by CCK8 assay
|
[PMID: 28523108] |
| MDA-MB-453 | IC50 |
120 nM
Compound: 5
|
Cytotoxicity against human MDA-MB-453 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth
Cytotoxicity against human MDA-MB-453 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth
|
[PMID: 35119278] |
| MDA-MB-453 | IC50 |
29 nM
Compound: 2; BLU9931
|
Inhibition of cell proliferation in human MDA-MB-453 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay
Inhibition of cell proliferation in human MDA-MB-453 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay
|
[PMID: 35549181] |
| NCI-H1299 | IC50 |
1.03 μM
Compound: 1a; BLU9931
|
Antiproliferative activity against human H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
|
[PMID: 33859803] |
| NCI-H1581 | IC50 |
>43.3 μM
Compound: 5
|
Cytotoxicity against human NCI-H1581 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth
Cytotoxicity against human NCI-H1581 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth
|
[PMID: 35119278] |
| RKO | IC50 |
19.67 μM
Compound: BLU9931
|
Antiproliferative activity against human RKO cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human RKO cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 37556948] |
| SMMC-7721 | IC50 |
6.617 μM
Compound: BLU9931
|
Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 33618175] |
| SW480 | IC50 |
12.72 μM
Compound: BLU9931
|
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 37556948] |
BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC50s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively[1].
BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4[1].
BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-453 and Hep 3B cells
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Concentration:0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
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Incubation Time:1 hour
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Result:Demonstrated potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 and Hep 3B cells.
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Cell Line:Hep 3B cells
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Concentration:100 nM
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Incubation Time:0 hour, 4 hours, 8 hour, 24 hours
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Result:Increased CYP7A1 mRNA expression. And the expression of the proliferative marker EGR1 was inhibited.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice injected with Hep 3B cells[1]
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Dosage:10 mg/kg, 30 mg/kg or 100 mg/kg
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Administration:Oral administration; twice every day; for 21 days
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Result:Resulted in dose-dependent growth inhibition of Hep 3B tumors. Prevented weight loss in a dose-dependent manner.
Chemical Information
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CAS No. 1538604-68-0
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Appearance Solid
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Masse moléculaire 509.38
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Formule C26H22Cl2N4O3
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Color White to light yellow
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SMILES
C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Theranostics
FGF19/SOCE/NFATc2 signaling circuit facilitates the self-renewal of liver cancer stem cells. [Abstract]2021 Mar 5;11(10):5045-5060. PMID: 33754043 -
Int J Biol Sci
2021 Jun 22;17(10):2576-2589. PMID: 34326695 -
Clin Transl Med
Spliceosomal profiling identifies EIF4A3 as a novel oncogene in hepatocellular carcinoma acting through the modulation of FGFR4 splicing. [Abstract]2022 Nov;12(11):e1102. PMID: 36419260 -
Eur J Med Chem
Design, synthesis, and biological evaluation of 1,6-naphthyridine-2-one derivatives as novel FGFR4 inhibitors for the treatment of colorectal cancer. [Abstract]2023 Nov 5:259:115703. PMID: 37556948 -
Commun Biol
Wnt/FGF20 signaling axis promotes migration of proximal blastema cell during tail regeneration of Gekko japonicus. [Abstract]2025 Dec 15. PMID: 41398307 -
Int J Oncol
Combination of FGFR4 inhibitor Blu9931 and 5-fluorouracil effects on the biological characteristics of colorectal cancer cells. [Abstract]2017 Nov;51(5):1611-1620. PMID: 29048661
BLU9931 purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Nov;51(5):1611-1620. [Abstract]
Western blot detection of the expression of related molecules including signal pathway (STAT3), apoptosis (cleaved caspase‑3), cell cycle (cyclin D1 and P27kip1) and epithelial-mesenchymal transition (E-cadherin and vimentin) in HCT116 and SW620 cells when treated by the single and combination of 5-FU and Blu9931.
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J Biol Chem
MAP3K4 promotes fetal and placental growth by controlling the receptor tyrosine kinases IGF1R/IR and Akt signaling pathway. [Abstract]2022 Sep;298(9):102310. PMID: 35921893 -
Clin Immunol
Inhibition of neutrophil extracellular traps via the FGF19/ERK/IL-8 axis enhances immune therapy in MSS colorectal cancer. [Abstract]2026 Apr:284:110664. PMID: 41565192 -
Solvant et solubilité
DMSO : 83.33 mg/mL (163.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9632 mL | 9.8159 mL | 19.6317 mL | 49.0793 mL |
| 5 mM | 0.3926 mL | 1.9632 mL | 3.9263 mL | 9.8159 mL | |
| 10 mM | 0.1963 mL | 0.9816 mL | 1.9632 mL | 4.9079 mL | |
| 15 mM | 0.1309 mL | 0.6544 mL | 1.3088 mL | 3.2720 mL | |
| 20 mM | 0.0982 mL | 0.4908 mL | 0.9816 mL | 2.4540 mL | |
| 25 mM | 0.0785 mL | 0.3926 mL | 0.7853 mL | 1.9632 mL | |
| 30 mM | 0.0654 mL | 0.3272 mL | 0.6544 mL | 1.6360 mL | |
| 40 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.2270 mL | |
| 50 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9816 mL | |
| 60 mM | 0.0327 mL | 0.1636 mL | 0.3272 mL | 0.8180 mL | |
| 80 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 mL | |
| 100 mM | 0.0196 mL | 0.0982 mL | 0.1963 mL | 0.4908 mL |