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Cat. No. Product Name CAS No. Information
PC-42888

BMS 777607

1025720-94-8

BMS 777607 is a potent, selective, orally efficacious inhibitor of Met kinase with IC50 of 3.9 nM, also potently inhibits Ron, Axl, Tyro-3 and Mer (IC50<15 nM), 40-fold selectivity over Lck, VEGFR-2 and TrkA/B; inhibits cell scattering activated by exogenous HGF in c-Met-expressing PC-3 and DU145 prostate cancer cells, suppresses HGF-stimulated cell migration and invasion with IC50 of <0.1 uM; potently blocks HGF-stimulated c-Met autophosphorylation and downstream activation of Akt and ERK at nanomolar level; demonstrates complete tumor stasis in Met-dependent GTL-16 human gastric carcinoma xenograft models.

Gastric Cancer

Phase 2 Clinical

PC-62101

DCC-2618

1442472-39-0

DCC-2618 (Ripretinib, DCC2618) is a potent, oral inhibitor of singly and doubly mutated KIT with IC50 of WT (IC50=4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM), D816V; also inhibits PDGFRα/β, KDR and cFMS, robustly inhibits exon 17, exon 9/13, exon 9/14, and exon 9/17 KIT mutants, as well as exon 11/17 KIT mutants; inhibits wild type and mutant KIT phosphorylation in cancer cells, demonstrates the potential to treat KIT mutant-driven cancers including GIST, systemic mastocytosis, AML, or melanoma.

Gastric Cancer

Phase 3 Clinical

PC-62100

Avapritinib

1703793-34-3

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively; displays weak inhibition against WT KIT with IC50 of 73 nM, >150-fold more potent on KIT D816V than several important kinase antitargets such as VEGFR2, SRC and FLT3; inhibits other well-characterized disease-driving KIT mutants both in vitro and in vivo in preclinical models, demonstrates marked activity in patients with diseases associated with KIT and PDGFRA (GIST) activation loop mutations.

Gastric Cancer

Phase 1 Clinical

PC-60082

Netazepide

155488-25-8

Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM; displays >5,000-fold selectivity over CCK-1 receptors; inhibits pentagastrin-induced gastric acid secretion in anesthetized rats (ED50=87 nM/kg), and shows potential for the treatment of gastroesophageal reflux disease (GERD); also inhibits gastric neuroendocrine enterochromaffin-like (ECL) cell hyperplasia and gastric carcinoid tumor development.

Gastric Cancer

Phase 2 Clinical

PC-42630

TSU-68

252916-29-3

TSU-68 (Orantinib, SU6668) is a small-molecule, ATP-competitiv inhibitor of angiogenic related RTKs KDR, PDGFRβ, FGFR1; inhibits receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands; significant growth inhibition of a diverse panel of human tumor xenografts after oral or i.p. administration.

Gastric Cancer

Phase 3 Discontinued

PC-45530

AMG-337

1173699-31-4

AMG-337 is a potent and selective inhibitor of MET with biochemical IC50 of 1 nM; inhibits of HGF-mediated MET phosphorylation in PC3 cells; shows desirable preclinical pharmacokinetics, significant inhibition of MET phosphorylation in mice, and robust tumor growth inhibition in a MET-dependent mouse efficacy model.

Gastric Cancer

Phase 2 Clinical

PC-45607

AZD-6738

1352226-88-0

AZD-6738 (AZD6738, Ceralasertib) is a potent and selective inhibitor of ATR with IC50 of 1 nM; shows no significant activity for ATM, DNA-PK and mTOR; inhibits ATR kinase-dependent CHK1 phosphorylation in cells (IC50=74 nM); enhances the therapeutic efficacy of cisplatin in xenograft models; orally active and bioavailable.

Gastric Cancer

Phase 2 Clinical

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