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Cat. No. Product Name CAS No. Information



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.

Liver Cancer

Phase 2 Clinical




AZD-4573 (AZD4573) is a potent and selective inhibitor of CDK9, with fast-off binding kinetics and high selectivity versus other kinases, including other CDK family kinases; AZD4573 exhibits a short half-life in multiple preclinical species and good solubility for intravenous administration; dose- and time-dependently decreases cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines; demonstrates in vivo efficacyin xenograft models derived from multiple haematological tumours.

Liver Cancer

Phase 1 Clinical




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.

Liver Cancer

Phase 2 Clinical



SF-1126 is a pan PI3K/BRD4 inhibitor, RGDS-conjugated LY294002 prodrug that exhibits increased solubility and binds to specific integrins; blocks expression levels of c-Myc in HCC cells, inhibits proliferation, cell cycle, apoptosis, PI3K/AKT/mTOR and Ras/Raf/MAPK pathway; shows significant antitumor activity in vivo.

Liver Cancer

Phase 1 Clinical




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.

Liver Cancer

Phase 3 Clinical




Linsitinib (ASP-7487, OSI-906) is a potent, selective, orally active, dual IGF-1R/insulin receptor inhibitor with IC50 of 35/75 nM, respectively; potently and selectively inhibits autophosphorylation of both human IGF-1R and IR, displays in vitro antiproliferative effects in a variety of tumor cell lines and shows robust in vivo anti-tumor efficacy in an IGF-1R-driven xenograft model.

Liver Cancer

Phase 3 Clinical




Tivantinib (ARQ-197) is a potent, selective, non-ATP-competitive inhibitor of c-Met with Ki of 355 nM; has no inhibition for EGFR, InsR, PDGFRα, FGFR1 and FGFR4 etc., only modest inhibition (35%) for Ron at 30 uM; inhibits constitutive c-Met phosphorylation in HT29 and MKN-45 cells, and HGF-induced c-Met phosphorylation in MDA-MB-231 and NCI-H441 cells with IC50 of 100-300 nM; shows antiproliferative activity against multiple cancer cell lines (IC50=0.03-30 uM); exerts tumor growth inhibition in multiple mouse xenograft; orally active.

Liver Cancer

Phase 3 Clinical

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