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Cat. No. Product Name CAS No. Information
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-42270

NCB-0846

1792999-26-8

The first orally available, small-molecule TNIK inhibitor with IC50 of 21 nM; also weakly inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK (IC80>0.1 uM); induces faster migration of TCF4 phosphorylated by TNIK at 0.1-0.3 uM, and completely inhibits at 3 uM; also reduces the expression of TNIK, AXIN2, cMYC, LRP6 and LRP5; abrogates colorectal cancer stemness, suppresses Wnt-driven intestinal tumorigenesis in Apc(min/+) mice.

Colon Cancer

Preclinical

PC-43790

Napabucasin

83280-65-3

Napabucasin (BBI-608) is a potent small-molecule inhibitor of STAT3 that has a broad spectrum of activity against stemness-high cancer cells (IC50=0.5-1.5 uM); blocks spherogenesis of cancer stem cells (CSC), but not hematopoietic stem cells; significantly reduces the expression of various stemness genes, including Nanog, Sox2, and Oct4 (POU5F1); significantly inhibits PaCa-2 xenograft tumor growth, and inhibits cancer relapse and metastasis.

Colon Cancer

Phase 3 Clinical

PC-45573

BGB-283

1446090-77-2

BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM); inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively; potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro; shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.

Colon Cancer

Preclinical

PC-35472

CKD-516

1188371-47-2 CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo; demonstrates potent cytotoxicity against several cancer cells including P-gp overexpressing MDR positive cell line (HCT15), also induces cell cycle arrest at G(2)/M phase, which is associated with strong inhibition of tubulin polymerization; shows antitumor efficacy against both murine tumors (CT26 and 3LL) and human xenogratfs (HCT116 and HCT15) in mice.

Colon Cancer

Phase 2 Clinical

PC-43483

Regorafenib hydrochloride

835621-07-3 Regorafenib hydrochloride (BAY73-4506) is a potent, orally active multikinase inhibitor that potently inhibits endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM); inhibits VEGFR1/2/3, PDGFRβ, FGFR1, KIT, RET and B-RAF etc.; exhibits potent dose-dependent TGI in various preclinical human xenograft models in mice.

Colon Cancer

Approved

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