colo205

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.

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.

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

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].