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Chemical Structure : H3B-6527
CAS No.: 1702259-66-2
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $178 | In stock | |
| 10 mg | $268 | In stock | |
| 25 mg | $458 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 629.543 | |
| Formula | C29H34Cl2N8O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Joshi JJ, et al. Cancer Res. 2017 Dec 15;77(24):6999-7013.
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