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Cat. No. Product Name CAS No. Information
PC-45812

Pelitinib

257933-82-7 A potent, selective, orally active, irreversible inhibitor of EGFR with IC50 of 80 nM; inhibits autophosphorylation of the cytoplasmic domain of HER-2 with IC50 of 1.23 uM; shows 1-3 orders of magnitude higher IC50 value for Src, Cdk4, c-Met, Raf, and MEK/ERK; inhibits proliferation in NHEK, A431, and MDA-468 cells (IC50= 61, 125, and 260 nM, respectively); potently inhibits the EGFR phosphorylation in A431 xenografts, suppresses tumorigenesis in APCMin/+ mice.

Lung Cancer

Phase 2 Clinical

PC-45892

Gefitinib hydrochloride

184475-55-6 A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM; inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM; blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM; significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth; has been used to treat advanced (or recurrent) non-small cell lung cancer.

Lung Cancer

Approved

PC-45891

Gefitinib

184475-35-2 A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM; inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM; blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM; significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth; has been used to treat advanced (or recurrent) non-small cell lung cancer.

Lung Cancer

Approved

PC-45428

Prexasertib dihydrochloride

1234015-54-3 A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models.

Lung Cancer

Phase 2 Clinical

PC-45427

Prexasertib

1234015-52-1 A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models.

Lung Cancer

Phase 2 Clinical

PC-45495

GSK-2879552

1401966-69-5 A potent, selective irreversible inhibitor of LSD1 with Ki app of 1.7 uM; shows good selectivity against LSD2, MAO-A, MAO-B, D-amino acid oxidase and LoxL2; exhibits growth inhibition (EC50=2-240 nM) in sensitive cell lines; orally bioavailable.

Lung Cancer

Phase 1 Clinical

PC-45893

Erlotinib

183321-74-6 A potent, selective inhibitor of EGFR with IC50 of 2 nM; reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM; inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentrations in cell culture and blocks cell cycle progression at the G1 phase; 100mg/kg completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice; orally active.

Lung Cancer

Approved

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