H3B-6527
- Product Name
- H3B-6527
- CAS No.
- 1702259-66-2
- Chemical Name
- H3B-6527
- Synonyms
- CS-2347;H3B-6527;H3 Biomedicine;H3B6527;H3B 6527;Eisai/H3 Biomedicine;H-3B-6527,H3B6527,H3B 6527;H3B-6527, 98%, a highly selective FGFR4 inhibitor with potent antitumour activity;N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide;2-Propenamide, N-[2-[[6-[[[(2,6-dichloro-3,5-dimethoxyphenyl)amino]carbonyl]methylamino]-4-pyrimidinyl]amino]-5-(4-ethyl-1-piperazinyl)phenyl]-
- CBNumber
- CB23146613
- Molecular Formula
- C29H34Cl2N8O4
- Formula Weight
- 629.54
- MOL File
- 1702259-66-2.mol
H3B-6527 Property
- Boiling point:
- 832.1±65.0 °C(Predicted)
- Density
- 1.373±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:50.0(Max Conc. mg/mL);79.42(Max Conc. mM)
- form
- A solid
- pka
- 11.00±0.70(Predicted)
N-Bromosuccinimide Price
- Product number
- 26072
- Product name
- H3B-6527
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $81
- Updated
- 2024/03/01
- Product number
- 26072
- Product name
- H3B-6527
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $238
- Updated
- 2024/03/01
- Product number
- 26072
- Product name
- H3B-6527
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $435
- Updated
- 2024/03/01
- Product number
- 26072
- Product name
- H3B-6527
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $887
- Updated
- 2024/03/01
- Product number
- 2308EF
- Product name
- H3B-6527
- Packaging
- 1mg
- Price
- $187
- Updated
- 2021/12/16
H3B-6527 Chemical Properties,Usage,Production
Biological Activity
H3B-6527 is a highly selective covalent FGFR4 inhibitor with IC50 < 1.2 nM, with >250-fold selectivity for FGFR4 over FGFR1-3 (IC50s of 320, 1290 and 1290 for FGFR1-3, respectively) 1060 nM).
in vitro
H3B-6527 has a strong inhibitory effect on FGFR4 with IC50 less than 1.2 nM. TAOK2, JNK2 and CSF1R were less sensitive to H3B-6527 treatment with IC50s of 690, >10000 and >10000 nmol/L, respectively. Treatment of Hep3B cells with H3B-6527 resulted in a concentration-dependent activation of caspase-3/7. It inhibits FGFR4 signaling, inhibits proliferation, and causes apoptosis in HCC cells.
in vivo
In a mouse model of Hep3B hepatocarcinoma xenografts, H3B-6527 had dose-proportional plasma exposure (greater than tumor exposure; doses tested were 30, 100, and 300 mg/kg). The pharmacodynamic response of H3B-6527 was detected, and it was found that CYP7A1 mRNA and pERK1/2 protein levels showed a concentration-dependent response, and higher concentrations would lead to a more durable response. In both subcutaneous Hep3B xenograft models and orthotopic xenograft models, oral administration of it (twice a day) significantly inhibited the growth of xenografts. Palbociclib enhanced the potency of it and promoted tumor regression in the JHH-7 model, whereas it single-agent administration only caused tumor growth arrest.