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Cat. No. Product Name CAS No. Information
PC-35813

CC-90003

1621999-82-3

CC-90003 (CC90003) is a potent and selective, covalent ERK1/2 inhibitor with IC50 of 10-20 nM, demonstrates excellent selectivity in a 258-kinase biochemical assay panel; potently inhibits 27 growth of KRAS mutant cell lines with GI50 of <1 uM, also is active against 28 of 37 (76%) KRAS-mutant cancer cell lines, shows cytotoxic effects in KRAS mutant PDAC, lung cancer and CRC cell lines, does not significantly inhibit proliferation of normal lung fibroblasts or bronchial epithelial cells; decreases colony formation ex-vivo and inhibits tumor growth in vivo of KRAS mutant PDX models, induces full regression and prevents regrowth of KRAS mutant Lung PDX model when combined with Docetaxel.

PC-62596

MK-8353 hydrochloride

1951448-73-9

MK-8353 hydrochloride (SCH-900353) is a highly potent, orally bioavailable, dual-specificity ERK1/2 inhibitor with IC50 of 23.0/8.8 nM, respectively; inhibits nonactivated ERK2 with IC50 of 0.5 nM, demonstrates excellent kinase selectivity over a 227-human kinase panel; decreases pERK1, pERK2, and ribosomal S6 kinase (pRSK) proteins, with complete suppression of pERK1 and pERK2 observed at 30 nM in A2058 cells, inhibits the in vitro proliferation of a panel of BRAFV600-mutant and RAS-mutant cancer cell lines; exhibits in vivo antitumor activity against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600 mutant SK-MEL-28 melanoma model.

Colon Cancer

Phase 1 Clinical

PC-62595

MK-8353

1184173-73-6

MK-8353 (SCH-900353) is a highly potent, orally bioavailable, dual-specificity ERK1/2 inhibitor with IC50 of 23.0/8.8 nM, respectively; inhibits nonactivated ERK2 with IC50 of 0.5 nM, demonstrates excellent kinase selectivity over a 227-human kinase panel; decreases pERK1, pERK2, and ribosomal S6 kinase (pRSK) proteins, with complete suppression of pERK1 and pERK2 observed at 30 nM in A2058 cells, inhibits the in vitro proliferation of a panel of BRAFV600-mutant and RAS-mutant cancer cell lines; exhibits in vivo antitumor activity against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600 mutant SK-MEL-28 melanoma model.

Colon Cancer

Phase 1 Clinical

PC-61978

KO-947

1695533-89-1

KO-947 is a potent and selective inhibitor of ERK1/2 kinase in biochemical, cellular and in vivo antitumor activity assays; blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling, including mutations in BRAF, NRAS or KRAS, at low nanomolar concentrations.

Solid Tumors

Phase 1 Clinical

PC-61973

LY-3214996

1951483-29-6

LY-3214996 is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays; potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines; demonstrates inhibition of cell proliferation, general sensitivitity against tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation; significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models.

Blood Cancer

Phase 1 Clinical

PC-35338

AZ6197

2023003-94-1 AZ6197 (AZ-6197) is a potent, selective, reversible inhibitor of ERK1/2 with IC50 of <0.3 nM (ERK2), inhibits pERK/pRSK with IC50 of 12/62 nM in A375 cells, respectively; demonstrates in vivo antitumor efficacy.
PC-35332

BAY-885

BAY-885 (BAY885) is a highly potent, selective ERK5 (MAPK7) inhibitor with IC50 of 40 nM, shows high selectivity over a panel of 357 kinases (Eurofins panel); strongly inhibits EGF-stimulated MEF2 transcriptional activity in MEF2 reporter assay with IC50 of 115 nM; despite its high potency, BAY-885 failed to inhibit the proliferation of cells with ERK5 genomic amplification (SN12C, SNU-449, MFM-223) or with constitutively active ERK5 signaling (BT-474, SK-BR-3).

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