colo205

Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。

SB-743921 hydrochloride (SB743921 HCl) 是一种有效的驱动蛋白纺锤体蛋白 KSP 抑制剂，Ki 值为 0.1 nM。

Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂，抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5 2.5 4.2 7 13 22 nM)，具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。

Regorafenib monohydrate 是一种新型口服多激酶抑制剂，对VEGFR1 2 3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。

Tubulin inhibitor 6 (iHAP1) 是一种微管蛋白抑制剂，抑制微管蛋白聚合，IC50为 0.87 μM。它抑制多种癌细胞系，抑制 K562 细胞生长，IC50为 840 nM。

Tubulin inhibitor 8是管蛋白和多种癌症细胞系的抑制剂，对管蛋白聚合和K562细胞生长具有抑制作用 ，IC50分别为0.73μM 和14nM。

Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂，通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性，可以诱导细胞凋亡、自噬。

Methotrexate (WR19039) 是一种叶酸类似物，一种二氢叶酸还原酶 DHFR 的抑制剂。Methotrexate 具有抗代谢、抗肿瘤和免疫抑制等活性，常用于类风湿关节炎和多种肿瘤的研究。

Everolimus (SDZ-RAD) 是 Rapamycin 的衍生物，是一种 mTOR1 抑制剂，具有选择性和口服活性。Everolimus 具有免疫抑制和抗肿瘤活性，可以抑制肿瘤细胞增殖、诱导细胞凋亡和自噬。

6-Hydroxycoumarin (6-hydroxychromen-2-one) 是一种香豆素。其中香豆素具有抗炎，支气管扩张，解热，血管扩张，抗氧化，抗菌，抗真菌，抑菌和抗肿瘤作用。

Cdc7-IN-12 (compound 1) 是 CDC7的有效抑制剂(IC50为 <1 nM)，在癌症研究中具有潜力。Cdc7-IN-12 在人结肠癌细胞COLO205 中表现出抗增殖活性，IC50为 100-1000 nM。

Cdc7-IN-18 (compound 1-2) is a highly effective inhibitor of the CDC7 enzyme. It has an IC 50 value of 1.29 nM for the Cdc7 DBF4 enzyme. In addition, this compound exhibits strong antiproliferative activities, with an IC 50 value of 53.62 nM in COLO205 cells [1].

SHR2415 是一种选择性的、高效的、口服具有活力的 ERK1 2 抑制剂。SHR2415 能够抑制 ERK1 (IC50: 2.8 nM) 和 ERK2 (IC50: 5.9 nM)。SHR2415 在 Colo205 细胞中表现出高效力 (IC50: 44.6 nM)。SHR2415 能够用于癌症的研究。

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) 为高效ABCB1抑制剂，可诱导细胞凋亡。含1-苯甲基咪唑基团，其对Colo205与Colo320细胞系展现出的IC50分别为1.26 μM与2.21 μM。

CDK4 6-IN-17（compound 12）为具有口服活性的CDK4 6抑制剂，在BE(2)细胞的IC50为10-100 nM。CDK4 6-IN-17在COLO205异种移植模型中有效抑制肿瘤生长。

COX-1 2-IN-4 为COX-1与COX-2酶的抑制剂，其IC50值分别为0.239 μM与0.191 μM。此化合物在对COLO205与B16F1癌细胞系表现出中等程度的抗癌活性，对应IC50值分别为30.79 μM与74.15 μM。