COLO205

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).

6-Hydroxycoumarin (6-hydroxychromen-2-one) exhibits cytotoxicity against human HL60, HCT116, COLO205 cells with activity value of 35 uM, 42 uM, 37 respectively. 6-Hydroxycoumarin is a human CA9, CA12 inhibitor.

Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor (IC50 < 1 nM) with potential applications in cancer research, demonstrating antiproliferative activity in COLO205 cells with an IC50 of 100-1000 nM [1].

Cdc7-IN-18 (compound 1-2) is a highly effective inhibitor of the CDC7 enzyme, with an IC50 value of 1.29 nM for the Cdc7 DBF4 enzyme. Additionally, this compound exhibits strong antiproliferative activities, with an IC50 value of 53.62 nM in COLO205 cells [1].

SHR2415 is a selective, potent, orally active inhibitor of ERK1 2. SHR2415 inhibits ERK1 (IC50: 2.8 nM) and ERK2 (IC50: 5.9 nM). SHR2415 exhibits high potency in Colo205 cells (IC50: 44.6 nM). SHR2415 can be used in cancer research.

BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol L (Colo205) to >8.5 micromol L (OV202). BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase Akt pathway, as evidenced by decreased Akt phosphorylation at Ser473. At doses that inhibited proliferation, the compound also caused a G0-G1 arrest and prevented nuclear accumulation of cyclin D1 in response to LR3 IGF-I. In Jurkat T-cell leukemia cells, this agent triggered apoptotic cell death via the mitochondrial pathway. BMS-554417 was orally bioavailable and significantly inhibited the growth of IGF1R-Sal tumor xenografts in vivo. BMS-554417 is a member of a novel class of IGF-IR insulin receptor inhibitors that have potential......

EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb.

ABCB1-IN-1 (compound 3) is a potent ABCB1 inhibitor that promotes cell apoptosis, featuring 1-benzylimidazole and exhibiting IC50 values of 1.26 μM for Colo205 cells and 2.21 μM for Colo320 cells, respectively [1].

CDK4 6-IN-17 (compound 12) is an orally bioavailable inhibitor of CDK4 6, exhibiting potent activity with IC50 values between 10-100 nM in BE(2) cells, and has demonstrated efficacy in inhibiting tumor growth in the COLO205 xenograft model [1].

COX-1 2-IN-4 (compound 2b) is a dual COX-1 and COX-2 inhibitor with IC50 values of 0.239 μM for COX-1 and 0.191 μM for COX-2, and demonstrates moderate anticancer activity with IC50 values of 30.79 μM against COLO205 cancer cell lines and 74.15 μM against B16F1 cancer cell lines [1].