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BLU9931

Catalog No. T2347 CAS 1538604-68-0

BLU9931 is the first selective small molecule inhibitor of FGFR4.

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BLU9931, CAS 1538604-68-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 30.00
5 mg	In stock	$ 48.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 128.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.85%

Purity: 98%

Purity: 96.958%

Purity: 96.33%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BLU9931 is the first selective small molecule inhibitor of FGFR4.
Targets&IC50	FGFR4:3 nM, FGFR3:150 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]
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]
Kinase Assay	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	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)

Molecular Weight	509.38
Formula	C26H22Cl2N4O3
CAS No.	1538604-68-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.09 mg/mL (10 mM)

References and Literature

1. Hagel M, et al. Cancer Discov. 2015, 5(4), 424-437.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Angiogenesis related Compound Library Cysteine Covalent Library

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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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BLU9931 1538604-68-0 Angiogenesis Tyrosine Kinase/Adaptors FGFR inhibit Inhibitor BLU 9931 BLU-9931 Fibroblast growth factor receptor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.