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Cat. No. Product Name CAS No. Information
PC-63139

TAK-931

1330782-76-7

TAK-931 (Simurosertib) is a potent, selective, ATP competitive and orally bioavailable inhibitor of Cdc7 with IC50 of <0.3 nM; prevents the initiation of DNA replication during mitosis, which causes cell cycle arrest and induces apoptosis, demonstrates antiproliferative activity with cancer cell lines and tumor growth inhibition (TGI) in murine ectopic xenograft models.

Colon Cancer

Phase 2 Clinical

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

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