BLU-9931 free base · Synonyms: BLU 9931 · BLU9931

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 inhibitor.

For research use only. Not for human or veterinary use.

Target FGFR

Research area Cancer

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Data Sheet SDS COA

BLU-9931 structure

CAS No.: 1538604-68-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 550.00	BP-01897-500mg	In stock	Get quote
1 g	USD 980.00	BP-01897-1g	In stock	Get quote
2 g	USD 1,650.00	BP-01897-2g	Inquire	Get quote
5 g	Inquire	BP-01897-5g	Inquire	Inquire

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Description

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.

Biological activity

In Vitro 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. 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. BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited. In Vivo BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models.

Identifiers

SMILES: COC1=CC(OC)=C(Cl)C(C2=CC3=CN=C(NC4=C(C)C=CC=C4NC(=O)C=C)N=C3C=C2)=C1Cl
InChIKey: TXEBNKKOLVBTFK-UHFFFAOYSA-N

Specifications

MW (average): 509.3840
Formula: C₂₆H₂₂Cl₂N₄O₃
CAS No.: 1538604-68-0
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Hagel M, et al. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37.

Same target

Search FGFR

Same research area

Search Cancer