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H3B-6527

Chemical Structure : H3B-6527

CAS No.: 1702259-66-2

H3B-6527 (H3B 6527;H3B6527)

Catalog No.: PC-60784Not For Human Use, Lab Use Only.

H3B-6527 is a potent, highly selective covalent FGFR4 inhibitor with IC50 of <1.2 nM, 250-fold selectivity over FGFR1-3 (IC50=320, 1290 and 1060 nM, respectively).

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Biological Activity

H3B-6527 is a potent, highly selective covalent FGFR4 inhibitor with IC50 of <1.2 nM, 250-fold selectivity over FGFR1-3 (IC50=320, 1290 and 1060 nM, respectively).
H3B-6527 displays liitle to no inhibitory activity against TAOK2, JNK2 and CSF1R (IC50=690, >10,000, and >10,000 nM).
H3B-6527 inhibits Hep3B celll viability with GI50 of 25 nM in ATP-based cell viability assay, inhibits proliferation and leads to apoptosis in HCC cell lines by inhibiting FGFR4 signaling.
H3B-6527 exhibits antitumor activity in the Hep3B human HCC xenograft mouse model.

Physicochemical Properties

M.Wt 629.543
Formula C29H34Cl2N8O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[2-[[6-[[[(2,6-Dichloro-3,5-dimethoxyphenyl)amino]carbonyl]methylamino]-4-pyrimidinyl]amino]-5-(4-ethyl-1-piperazinyl)phenyl]-2-propenamide

References

1. Joshi JJ, et al. Cancer Res. 2017 Dec 15;77(24):6999-7013.

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