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Cat. No. Product Name CAS No. Information
PC-42551

MK 2206 dihydrochloride

1032350-13-2 A potent, orally active allosteric Akt inhibitor with IC50 of 5/12 nM for Akt1/Akt2 respectively; shows 5-fold less potent against human Akt3 (IC50=65 nM); synergistically inhibits cell proliferation of human cancer cell lines in combination with erlotinib or lapatinib in vitro; suppresses the Akt phosphorylation that is induced by carboplatin and gemcitabine.

Colon Cancer

Phase 2 Clinical

PC-45828

PD-184352

212631-79-3 A potent, ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, displays 100-fold more selective for MEK1/2 than MEK5; reduces pMAPK levels in multiple tumor cells, prevents cell cycle progression and induces G1 block; suppresses growth of colon tumors in vivo.

Colon Cancer

Phase 2 Discontinued

PC-45859

Linifanib

796967-16-3 A potent multi-RTKs inhibitor of members of VEGFR and PDGFR families with IC50 of 4/3/3/14/4/66/190/170 nM for KDR/FLT1/CSF1R/KIT/FLT3/PDGFRβ/FLT4/Tie2, respectively; much less active (IC50>10 uM) against other nonrelated tyrosine kinases, such as steroid receptor coactivator and EGFR; inhibits RTK phosphorylation (IC50=2, 4, and 7 nM for PDGFRβ, KDR, and CSF-1R, respectively) and VEGF-stimulated proliferation (IC50=0.2 nM for human endothelial cells); exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models (ED50=1.5-5 mg/kg, twice daily).

Colon Cancer

Phase 2 Discontinued

PC-42531

Regorafenib monohydrate

1019206-88-2 A potent multikinase inhibitor that potently inhibits these 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; orally active.

Colon Cancer

Approved

PC-42530

Regorafenib

755037-03-7 A potent multikinase inhibitor that potently inhibits these 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; orally active.

Colon Cancer

Approved

PC-45342

WNT-974

1243244-14-5 A potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1 nM in the PORCN radioligand binding assay; potently inhibits Wnt signaling with IC50 of 0.4 nM, with no major cytotoxicity; reduces Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2; is potent and efficacious in multiple tumor models at well-tolerated doses in vivo.

Colon Cancer

Phase 2 Clinical

PC-45746

Fruquintinib

1194506-26-7 A potent and highly selective small molecule inhibitor of VEGFR1/2/3 with IC50 of 33/3/5/0.5 nM, respectively; weakly inhibits RET, FGFR-1 and c-kit kinases; demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50 of 0.6 nM and 1.7 nM, respectively; suppresses tumor growth inhibition in a panel of tumor xenograft and patient derive xenograft models in mouse; orally active.

Colon Cancer

Phase 3 Clinical

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