Liver cancer is a type of cancer that starts in the liver. Cancer starts when cells in the body begin to grow out of control. When cancer starts in the liver, it is called liver cancer. Each year in the United States, about 33,000 people get liver cancer, and about 27,000 people die from the disease. The percentage of Americans who get liver cancer has been rising for several decades.
Many liver cancer cases are related to hepatitis B virus or hepatitis C virus infections. Most people don’t know they have the virus.
Other behaviors and conditions that increase risk for getting liver cancer are--
~Excessive alcohol use.
~Cirrhosis (scarring of the liver, which can also be caused by hepatitis and alcohol use).
~Having hemochromatosis, a condition where the body takes up and stores more iron than it needs.
~Eating foods that have aflatoxin (a fungus that can grow on foods, such as grains and nuts that have not been stored properly).
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FGF-401 (NVP-FGF401, Roblitinib, FGF401) is a first-in-class, potent, highly selective FGFR4 inhibitor with IC50 of 1.1 nM; shows >1,000-fold selectivity against of panel of 65 kinases and in a kinome of 456 kinases; potently inhibits phospho-FGFR4 in vivo, exhibits anti-tumor activity in s several xenograft animal models.
BLU-554 (Fisogatinib, BLU554) is a novel potent, highly selective and orally bioavailable inhibitor of FGFR4 designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation; targets FGFR4 while sparing other members of the FGFR family and showing little to no inhibition of all other kinases.
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); displays liitle to no inhibitory activity against TAOK2, JNK2 and CSF1R (IC50=690, >10,000, and >10,000 nM); 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; exhibits antitumor activity in the Hep3B human HCC xenograft mouse model.
2-Cl-IB-MECA (Chloro-IB-MECA, CF-102, Namodenoson) is a potent, selective A3 adenosine receptor agonist with Ki of 0.33 nM, 2500- and 1400-fold selectivity over A1 and A2a receptors; also displays 46,000-fold selectivity versus the Na(+)-independent adenosine transporter; inhibits adenylate cyclase via rat A3 receptors in CHO cells (IC50=67 nM); induces apoptosis in HL-60 cells at concentrations of <30 uM, significantly induced Ca(2+) release from intracellular Ca(2+) pools followed by Ca(2+) influx; increases plasma histamine concentrations in conscious rats.
PLB-1001 (Bozitinib, PLB1001, CBI-3103, CBT-101) is a potent, highly selective, ATP-competitive, BBB-permeable MET kinase inhibitor, potently inhibits MET activity by 95.1% at 2 uM; Similar with crizotinib, PLB-1001 inhibited the phosphorylation of MET and STAT3, indicating a robust inhibitory effect of PLB-1001 on MET and its downstream signaling pathways; demonstrates remarkable potency in selectively inhibiting MET-altered tumor cells (METex14) in preclinical models; also exhibits clinical potential for precisely treating gliomas.
OBI-3424 (AST-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent; OBI-3424 is a nitro-benzene prodrug of N,N’-bisethylenephosphoramidate, demonstrates in vivo efficacy against preclinical xenograft models of pediatric T-ALL.
Foslinanib sodium (TRX-818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities, induces cancer cell apoptosis and inhibits cancer cell proliferation; also prevents tumor cell VM by blocking the formation of vasculogenic-like tubular structures through an as of yet undetermined mechanism of action.
Foslinanib (TRX-818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities, induces cancer cell apoptosis and inhibits cancer cell proliferation; also prevents tumor cell VM by blocking the formation of vasculogenic-like tubular structures through an as of yet undetermined mechanism of action.
Seocalcitol is vitamin D3 analogue with potential antineoplastic activity. Seocalcitol binds to and activates the vitamin D receptor, a cytoplasmic polypeptide expressed in normal vitamin D responsive tissues, but also overexpressed in certain cancers including hepatocellular carcinoma and pancreatic cancer.
Derazantinib (ARQ-087) is a novel potent, ATP competitive multi-kinase inhibitor with IC50 of FGFR1/2/3 with IC50 of 1.8-4.5 nM; also inhibits FGFR4, Src, Abl, RET, etc. (IC50<50 nM); inhibits FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK), shows potent anti-proliferative effect in cell lines driven by FGFR dysregulation; shows tumor growth inhibition in vivo in xenograft tumor models.
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