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H3B-6527

Catalog No. T7738 CAS 1702259-66-2

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma, with antineoplastic activity.

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H3B-6527, CAS 1702259-66-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 81.00
2 mg	In stock	$ 138.00
5 mg	In stock	$ 191.00
10 mg	In stock	$ 332.00
25 mg	In stock	$ 558.00
50 mg	In stock	$ 788.00
100 mg	In stock	$ 1,120.00
1 mL * 10 mM (in DMSO)	In stock	$ 297.00

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Purity: 99.85%

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Description	H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma, with antineoplastic activity.
In vitro	H3B-6527, a highly selective covalent FGFR4 inhibitor, through structure-guided drug design. Studies in a panel of 40 HCC cell lines and 30 HCC PDX models showed that FGF19 expression is a predictive biomarker for H3B-6527 response. Moreover, coadministration of the CDK4/6 inhibitor palbociclib in combination with H3B-6527 could effectively trigger tumor regression in a xenograft model of HCC[1].?FGFR4 is frequently overexpressed in ESCC tissue and cell lines. in vitro assays have shown that blocking FGFR4 by a specific blocker, H3B-6527, significantly decreases proliferation, invasion, and migration, and alters epithelial-mesenchymal transition markers in ESCC cells. In addition, FGFR4 blockade is associated with the induction of apoptosis and affects PI3K/Akt and MAPK/ERK pathways[2].
Cell Research	Immunohistochemistry and Western blotting were used to detect FGFR4 expression in ESCC samples and cell lines. Cell counting kit-8, and clonogenic, transwell, flow cytometric, and tumor xenograft in nude mice assays were utilized to determine the effect of blocking FGFR4 in proliferation, invasion, migration, and apoptosis of ESCC cells[2].

Molecular Weight	629.54
Formula	C29H34Cl2N8O4
CAS No.	1702259-66-2

Storage

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

Solubility Information

DMSO: 6.3 mg/mL (10 mM)

References and Literature

1. Joshi, Jaya Julie, Coffey, Heather, Corcoran, Erik,et al. H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma[J]. Cancer Research, 77(24):6999-7013. 2. Zhongwei, Xin, Xuemin, et al. Blocking FGFR4 exerts distinct anti-tumorigenic effects in esophageal squamous cell carcinoma.[J]. Thoracic cancer, 2018.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Highly Selective Inhibitor Library Kinase Inhibitor Library Anti-Prostate Cancer Compound Library Apoptosis Compound Library Anti-Liver Cancer Compound Library Anti-Breast Cancer Compound Library NO PAINS Compound Library

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Keywords

H3B-6527 1702259-66-2 Angiogenesis Tyrosine Kinase/Adaptors FGFR H3B6527 H-3B-6527 H3B 6527 inhibitor inhibit

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