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TW-37
TW-37是一种新型的非肽类抑制剂，作用于重组Bcl-2，Bcl-xL和Mcl-1，无细胞试验中Ki分别为0.29 μM， 1.11 μM和0.26 μM。
TW-37 Chemical Structure
CAS: 877877-35-5
产品质控
批次：
纯度：
99.78%
99.78
TW-37相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| human RPMI-2650 cell | Growth inhibition assay | Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=0.23831 μM | |||
| human MDA-MB-361 cell | Growth inhibition assay | Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=0.2264 μM | |||
| human A2780 cell | Growth inhibition assay | Inhibition of human A2780 cell growth in a cell viability assay, IC50=0.21846 μM | |||
| human SW1783 cell | Growth inhibition assay | Inhibition of human SW1783 cell growth in a cell viability assay, IC50=0.21301 μM | |||
| human NY cell | Growth inhibition assay | Inhibition of human NY cell growth in a cell viability assay, IC50=0.17762 μM | |||
| human LoVo cell | Growth inhibition assay | Inhibition of human LoVo cell growth in a cell viability assay, IC50=0.16093 μM | |||
| human HT-144 cell | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay, IC50=0.15201 μM | |||
| human MDA-MB-453 cell | Growth inhibition assay | Inhibition of human MDA-MB-453 cell growth in a cell viability assay, IC50=0.15188 μM | |||
| human Daoy cell | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50=0.14073 μM | |||
| human MG-63 cell | Growth inhibition assay | Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.11248 μM | |||
| human SW756 cell | Growth inhibition assay | Inhibition of human SW756 cell growth in a cell viability assay, IC50=0.11236 μM | |||
| human SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.1107 μM | |||
| human MDA-MB-231 cell | Growth inhibition assay | Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=0.10807 μM | |||
| human GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=98.69 nM | |||
| human A204 cell | Growth inhibition assay | Inhibition of human A204 cell growth in a cell viability assay, IC50=97.84 nM | |||
| human A375 cell | Growth inhibition assay | Inhibition of human A375 cell growth in a cell viability assay, IC50=88.83 nM | |||
| human HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=87.01 nM | |||
| human HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay, IC50=84.71 nM | |||
| human HEC-1 cell | Growth inhibition assay | Inhibition of human HEC-1 cell growth in a cell viability assay, IC50=81.37 nM | |||
| human U-87-MG cell | Growth inhibition assay | Inhibition of human U-87-MG cell growth in a cell viability assay, IC50=82.24 nM | |||
| human NB14 cell | Growth inhibition assay | Inhibition of human NB14 cell growth in a cell viability assay, IC50=76.45 nM | |||
| human MC-IXC cell | Growth inhibition assay | Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=75.33 nM | |||
| human LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=72.85 nM | |||
| human YH-13 cell | Growth inhibition assay | Inhibition of human YH-13 cell growth in a cell viability assay, IC50=70.59 nM | |||
| human CP50-MEL-B cell | Growth inhibition assay | Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50=69.59 nM | |||
| human SK-MEL-5 cell | Growth inhibition assay | Inhibition of human SK-MEL-5 cell growth in a cell viability assay, IC50=69.25 nM | |||
| human NCI-H1581 cell | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=67.64 nM | |||
| human SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=58.9 nM | |||
| human SF126 cell | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50=57.07 nM | |||
| human A673 cell | Growth inhibition assay | Inhibition of human A673 cell growth in a cell viability assay, IC50=53.85 nM | |||
| human HCT-116 cell | Growth inhibition assay | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=52.66 nM | |||
| human A427 cell | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50=44.69 nM | |||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=52.13 nM | |||
| human SK-MEL-30 cell | Growth inhibition assay | Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=37.97 nM | |||
| human AGS cell | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50=37.53 nM | |||
| human UACC-62 cell | Growth inhibition assay | Inhibition of human UACC-62 cell growth in a cell viability assay, IC50=34.35 nM | |||
| human SAS cell | Growth inhibition assay | Inhibition of human SAS cell growth in a cell viability assay, IC50=33.18 nM | |||
| human HuH-7 cell | Growth inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=32.82 nM | |||
| human NB7 cell | Growth inhibition assay | Inhibition of human NB7 cell growth in a cell viability assay, IC50=29.28 nM | |||
| human YKG-1 cell | Growth inhibition assay | Inhibition of human YKG-1 cell growth in a cell viability assay, IC50=29.76 nM | |||
| human SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=28.68 nM | |||
| human Hs-578-T cell | Growth inhibition assay | Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=23.59 nM | |||
| human BHT-101 cell | Growth inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=21.83 nM | |||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=15.17 nM | |||
| human GCIY cell | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay, IC50=20.83 nM | |||
| human A549 cell | Growth inhibition assay | Inhibition of human A549 cell growth in a cell viability assay, IC50=14.09 nM | |||
| human CHL-1 cell | Growth inhibition assay | Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=11.9 nM | |||
| human Ca9-22 cell | Growth inhibition assay | Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50=3.82 nM | |||
| human JAR cell | Growth inhibition assay | Inhibition of human JAR cell growth in a cell viability assay, IC50=2.6 nM | |||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | TW-37是一种新型的非肽类抑制剂，作用于重组Bcl-2，Bcl-xL和Mcl-1，无细胞试验中Ki分别为0.29 μM， 1.11 μM和0.26 μM。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | TW-37是新型非肽类小分子 Bcl-2抑制剂。 | ||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | TW-37靶向作用于Bcl-2 中与促凋Bcl-2蛋白结合的亡BH3结合槽, 作用于Bcl-2和Mcl-1比作用于Bcl-xL亲和力和选择性高， Ki 分别为0.29 μM, 0.26 μM 和1.11 μM。在体外, TW-37作用于从淋巴瘤患者体内得到的原发性细胞 和抗de novo化疗的WSU-DLCL2 淋巴瘤细胞系，具有抗增殖和促凋亡效果，而对正常外周血淋巴细胞则没效果。[1] TW-37作用于内皮细胞，抑制细胞生长和细胞死亡，IC50约为1.8 μM，但是相同浓度TW-37处理成纤维细胞则没效果。此外, TW37按相同的低浓度作用于MCF-7, LNCaP, 和SLK肿瘤细胞系，具有抗增殖效果，所用药物浓度比抑制内皮细胞生长所需浓度低。[2] |
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|---|---|---|---|---|
| 激酶实验 | 重组 Bcl-2,Bcl-XL,和 Mcl-1蛋白荧光偏振结合实验 | |||
| 为了进行次实验,使用 6-羧基荧光琥珀酰亚胺酯(FAM-Bid)标记的Bid 衍生的21个残基 BH3肽 QEDIIRNIARHLAQVGDSMDR，及人Bcl-2,Bcl-X L,和 Mcl-1衍生的重组蛋白。FAM-Bid 作用于Bcl-2, Bcl-XL和Mcl-1蛋白时，Ki 分别为11 nM ,25 nM, 和 5.7 nM。Bcl-XL竞争性结合实验与Bcl-2实验一样，除了以下不同：30 nM Bcl-XL 蛋白和2.5 nM FAM-Bid肽溶于以下实验[50 mM Tris-Bis (pH 7.4) 和0.01%牛gamma-球蛋白]。 | ||||
| 细胞实验 | 细胞系 | HDMECs | ||
| 浓度 | 0到100 μM | |||
| 孵育时间 | 96小时 | |||
| 方法 | 进行sulforhodamine B(SRB)毒性实验。通过分析生长曲线而测定毒性实验最佳细胞密度。HDMECs接种在96孔板上，使其粘附过夜。药物在EGM2-MV中稀释，然后分层加到细胞中cells,按指定时间温育。另外, HDMECs 与TW37和0 到100 ng/mL重组人VEGF(rhVEGF)165或0 到100 ng/mL 重组人CXCL8共温育。在板上加入冰冻三氯乙酸 (终浓度为10%)，与细胞在4oC下温育1小时。加入溶于1%乙酸的0.4% SRB，对细胞蛋白进行染色，然后在室温下温育30分钟。使用1% 乙酸冲洗，移除未结合的SRB，然后烘干实验板。结合的SRB再溶解在10 mM 无缓冲 Tris-碱中，然后使用酶标仪在 560 nm测定吸光值。每组实验进行至少三次独立重复实验，获得实验数据。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | TW-37按40 mg/kg最大耐受剂量(MTD)单独静脉注射给药SCID小鼠，注射三次，增强CHOP方案抑制肿瘤的效果。[1] TW-37静脉注射处理含人血管新生的SCID小鼠，通过降低功能性人血管 密度而产生抗血管生成效果。[2] TW-37与MEK抑制剂的联合用药，协同性的抑制了小鼠中黑色素瘤细胞的生长。[3] |
|
|---|---|---|
| 动物实验 | Animal Models | 移植了SK-Mel-147黑色素瘤的小鼠 |
| Dosages | ~40 mg/kg | |
| Administration | 静脉注射或腹腔注射 | |
|
化学信息&溶解度
| 分子量 | 573.7 | 分子式 | C33H35NO6S |
| CAS号 | 877877-35-5 | SDF | Download TW-37 SDF |
| Smiles | CC(C)C1=CC=CC=C1CC2=CC(=C(C(=C2O)O)O)C(=O)NC3=CC=C(C=C3)S(=O)(=O)C4=CC=CC=C4C(C)(C)C | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 115 mg/mL ( (200.45 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 4 mg/mL (6.97 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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