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H3B-6527

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Catalog No. T7738Cas No. 1702259-66-2

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

H3B-6527

H3B-6527

🥰Excellent
Purity: 97.45%
Catalog No. T7738Cas No. 1702259-66-2
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma, with antineoplastic activity.
Pack SizePriceAvailabilityQuantity
1 mg$64In Stock
5 mg$172In Stock
10 mg$289In Stock
25 mg$558In Stock
50 mg$788In Stock
100 mg$1,120In Stock
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Purity:97.45%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight629.54
FormulaC29H34Cl2N8O4
Cas No.1702259-66-2
SmilesCCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)c(NC(=O)C=C)c1
Relative Density.1.373 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 6.3 mg/mL (10 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5885 mL7.9423 mL15.8846 mL79.4231 mL
5 mM0.3177 mL1.5885 mL3.1769 mL15.8846 mL
10 mM0.1588 mL0.7942 mL1.5885 mL7.9423 mL

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