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Cat. No. Product Name CAS No. Information
PC-35250

AZD-4573

2057509-72-3

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

PC-43007

2-Cl-IB-MECA

163042-96-4

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
PC-60413

SF-1126

936487-67-1

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

PC-42436

Linsitinib

867160-71-2

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

PC-45842

Tivantinib

905854-02-6

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

PC-44038

Tepotinib

1100598-32-0

Tepotinib (EMD-1214063) is a potent and highly selective c-Met inhibitor with IC50 of 3 nM; shows selectivity versus a panel of 242 human kinases; inhibits c-Met phosphorylation and downstream signaling in a dose-dependent fashion; induces regression of human tumors in murine xenograft models.

Liver Cancer

Phase 2 Clinical

PC-42406

FGF-401

1708971-55-4

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.

Liver Cancer

Phase 2 Clinical

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