GLPBio

BLU-554

Catalog No.: GC19075Purity:>99.50%Synonyms: BLU-554
COASDSData Sheet
BLU-554 is a selective inhibitor of fibroblast growth factor receptor 4 (FGFR4) (IC50 = 5nM).

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BLU-554
Cas No.: 1707289-21-1
10mM (in 1mL DMSO)In Stock
$97.00
1
1mgIn Stock
$40.00
1
5mgIn Stock
$88.00
1
10mgIn Stock
$140.00
1
25mgIn Stock
$238.00
1
50mgIn Stock
$357.00
1
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Description

BLU-554 is a selective inhibitor of fibroblast growth factor receptor 4 (FGFR4) (IC50 = 5nM) [1]. BLU-554 selectively inhibits the activity of FGFR4 kinase, blocking the FGF19-FGFR4 pathway, thereby inhibiting the proliferation and growth of tumor cells [2]. BLU-554 is commonly used to treat hepatocellular carcinoma [3-4].

In MKN-45 cells, BLU-554 (0.05μM, 0.5μM, 5μM; 48h) inhibit the proliferation of gastric cancer cell line MKN-45 [5]. In HuH-7 and JHH-7 cells, BLU-554 (0-1250nM; 12h, 48h) can effectively inhibit FGFR4 activity in cells [6]. in PC9-4X cells, BLU-554 (1μM; 72h) reduces the IC50 of gefitinib [7].

In SW480-ELF4 cells subcutaneous tumor mice model, combination of BLU-554 (10mg/kg; ig; 9 weeks) and KX2-391 significantly inhibits ELF4-mediated CRC metastasis [8]. In Hepa1-6-ETV4 xenograft mice models, BLU-554 (100mg/kg; ig; 9 weeks) monotherapy partially reduced lung metastasis and lengthened the OS of the Hepa1-6-ETV4 [9].

References:
[1]. Dogan-Topal B, Li W, Schinkel AH, et al. Quantification of FGFR4 inhibitor BLU-554 in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. Journal of Chromatography B. 2019 Mar 15; 1110: 116-123.
[2]. Subbiah V, Pal SK. Precision oncology for hepatocellular cancer: Slivering the liver by FGF19–FGFR4–KLB pathway inhibition. Cancer discovery. 2019 Dec 1; 9(12): 1646-1649.
[3]. Kim RD, Sarker D, Meyer T, et al. First-in-human phase I study of fisogatinib (BLU-554) validates aberrant fibroblast growth factor 19 signaling as a driver event in hepatocellular carcinoma. Cancer Discovery. 2019; 9(12): 1696-1707.
[4]. Kim R, Sarker D, Macarulla T, et al. Phase 1 safety and clinical activity of BLU-554 in advanced hepatocellular carcinoma (HCC). Annals of Oncology. 2017 Sep 1; 28: v122.
[5]. Zhang X, Zhang X, Han R, et al. BLU-554, a selective inhibitor of FGFR4, exhibits anti-tumour activity against gastric cancer in vitro. Biochemical and Biophysical Research Communications. 2022 Mar 5; 595: 22-27.
[6]. Tao Z, Cui Y, Xu X, et al. FGFR redundancy limits the efficacy of FGFR4-selective inhibitors in hepatocellular carcinoma. Proceedings of the National Academy of Sciences. 2022 Oct 4; 119(40): e2208844119.
[7]. Liu D, Liu H, Gan J, et al. LY2874455 and abemaciclib reverse FGF3/4/19/CCND1 amplification mediated gefitinib resistance in NSCLC. Frontiers in Pharmacology. 2022 Jun 23; 13: 918317.
[8]. Chen X, Chen J, Feng W, et al. FGF19-mediated ELF4 overexpression promotes colorectal cancer metastasis through transactivating FGFR4 and SRC. Theranostics. 2023 Feb 22; 13(4): 1401.
[9]. Xie M, Lin Z, Ji X, et al. FGF19/FGFR4-mediated elevation of ETV4 facilitates hepatocellular carcinoma metastasis by upregulating PD-L1 and CCL2. Journal of Hepatology. 2023 Jul 1; 79(1): 109-125.

Protocol

Cell experiment [1]:

Cell lines

MKN-45 cells

Preparation Method

The cells were digested, resuspended, counted, and plated at a density of 5000 cells/well. After adherence, cells were incubated with the two inhibitor solutions configured as previously mentioned for 48h, and media in the 96-well plate (100μL/well) was replaced. BLU-554 was mixed with dimethyl sulfoxide to make a 5mg/mL mother liquor, vortexed until completely dissolved. The solution was diluted with complete medium to 0.05, 0.5, and 5μM when used, vortexed to mix, and stored.

Reaction Conditions

0.05μM, 0.5μM, 5μM; 48h

Applications

BLU-554 inhibit the proliferation of gastric cancer cell line MKN-45.
Animal experiment [2]:

Animal models

SW480-ELF4 cells subcutaneous tumor mice model

Preparation Method

Six-week-old BALB/c nude mice were randomly divided into groups (10 mice per group) to establish a tail vein or intrasplenic injection metastasis model, and 1×10⁶ or 2×10⁶ luciferase-labeled CRC cells were injected, respectively. Treatment began 1 week after inoculation, and BLU-554 (10mg/kg), KX2-391 (15mg/kg) or combined drugs were given by gavage daily, and a vehicle control group was set up. D-luciferin was injected intraperitoneally every week for IVIS imaging to record tumor progression. Mice were killed after 9 weeks to evaluate lung and liver metastasis and survival time.

Dosage form

10mg/kg; ig; 9 weeks

Applications

Combination of BLU-554 and KX2-391 significantly inhibits ELF4-mediated CRC metastasis.

References:
[1]. Zhang X, Zhang X, Han R, et al. BLU-554, a selective inhibitor of FGFR4, exhibits anti-tumour activity against gastric cancer in vitro. Biochemical and Biophysical Research Communications. 2022 Mar 5; 595: 22-27.
[2]. Chen X, Chen J, Feng W, et al. FGF19-mediated ELF4 overexpression promotes colorectal cancer metastasis through transactivating FGFR4 and SRC. Theranostics. 2023 Feb 22; 13(4): 1401.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1707289-21-1
Synonyms
BLU-554
SMILES
C=CC(N[C@@H]1[C@H](NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)COCC1)=O
Molecular Formula
C24H24Cl2N4O4
Molecular Weight
503.38
Solubility
DMSO : ≥ 25 mg/mL (49.66 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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