An FGFR4 inhibitor (IC50 = 50s = 320

H3B-6527 – 25 mg

Brand:
Cayman
CAS:
1702259-66-2
Storage:
-20
UN-No:
Non-Hazardous - /

H3B-6527 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 50s = 320, 1,290, and 1,060 nM, respectively), as well as TAOK2, JNK2, and CSF1R (IC50s = 690, >10,000, and >10,000 nM, respectively). H3B-6527 increases the expression of the cytochrome P450 (CYP) isoform CYP7A1 and decreases phosphorylation of ERK1/2 in Hep3B hepatocellular carcinoma (HCC) cells in a concentration-dependent manner, indicating inhibition of the FGF19-FGFR4 signaling pathway. It also decreases cell growth (GI50 = 25 nM) and increases caspase-3/7 activity in Hep3B HCC cells. H3B-6527 selectively inhibits cell growth in HCC cell lines that express high levels of FGF19 and have high FGF19 protein levels. It reduces tumor growth in a Hep3B HCC mouse xenograft model, when administered at doses of 100 and 300 mg/kg, and in patient-derived xenograft models with high FGF19 expression. H3B-6527, in combination with PD 0332991 (palbociclib; Item No. 16273), induces tumor stasis in a JHH-7 mouse xenograft model.  

 

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SKU: 26072 - 25 mg Category:

Description

An FGFR4 inhibitor (IC50 = 50s = 320, 1,290, and 1,060 nM, respectively), as well as TAOK2, JNK2, and CSF1R (IC50s = 690, >10,000, and >10,000 nM, respectively); decreases cell growth (GI50 = 25 nM) and increases caspase-3/7 activity in Hep3B HCC cells; selectively inhibits cell growth in HCC cell lines that express high levels of FGF19; reduces tumor growth in a Hep3B HCC mouse xenograft model at 100 and 300 mg/kg

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

Synonyms: 

Molecular weight: 629.5

CAS: 1702259-66-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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