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。

Tunlametinib是高选择性口服MEK1/MEK2激酶抑制剂（对MEK1的IC50为1.9 nM），通过阻断RAS-RAF-MEK-ERK致癌信号通路诱导肿瘤细胞周期阻滞与凋亡。对BRAF V600E或KRAS G12C等突变型肿瘤细胞具有强抑制活性，与BRAF/KRASG12C/SHP2抑制剂及多西他赛（Docetaxel）联用呈现协同效应，目前已应用于黑色素瘤、结直肠癌及非小细胞肺癌等RAS/RAF驱动型肿瘤的靶向治疗。

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。