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TW-37

TW-37

产品编号 T6281   CAS 877877-35-5
别名: TW 37

TW-37 是重组 Bcl-2、Bcl-xL 和 Mcl-1 的非肽抑制剂,Ki 值分别为 0.26、0.29和1.11μM

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TW-37 Chemical Structure
TW-37, CAS 877877-35-5
规格 价格/CNY 货期 数量
1 mg ¥ 262 现货
2 mg ¥ 379 现货
5 mg ¥ 663 现货
10 mg ¥ 955 现货
25 mg ¥ 1,830 现货
50 mg ¥ 3,320 现货
100 mg ¥ 4,750 待询
1 mL * 10 mM (in DMSO) ¥ 838 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: TW-37 (T6281)
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纯度: 98%
纯度: 97.06%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 TW-37 is an nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 (Ki: 0.29/1.11/0.26 μM).
靶点活性 BCL-XL:1.11 μM(Ki), BCL2:0.29 μM(Ki), MCL1:0.26 μM(Ki)
体外活性 TW-37 targets the BH3-binding groove in Bcl-2 where proapoptotic Bcl-2 proteins bind, and shows higher affinity and selectivity for Bcl-2 and Mcl-1 over Bcl-xL with Ki values of 0.29 μM, 0.26 μM and 1.11 μM, respectively. [1] In vitro, TW-37 shows significant anti-proliferative and pro-apoptotic effect in a de novo chemo-resistant WSU-DLCL2 lymphoma cell line and primary cells obtained from a lymphoma patient without effects on normal peripheral blood lymphocytes. [1] TW-37 exhibits the inhibitory effect on both cell growth and cell death in endothelial cell with IC50 of approximately 1.8 μM without effect on the fibroblasts exposed to the same concentration range as the endothelial cells. In addition, TW37 also shows the anti-proliferation effects in MCF-7, LNCaP, and SLK tumor cell lines with the same or lower concentration range than those required to inhibit endothelial cell growth. [2]
体内活性 TW-37 shows a maximum tolerated dose (MTD) of 40 mg/kg for three i.v. injections in severe combined immunodeficient (SCID) mice when given alone, and enhances tumor inhibitory effect of cyclophosphamide-doxorubicin-vincristine-prednisone (CHOP) regimen. [1] TW-37, administrated by i.v. produces the antiangiogenic effect by decreasing the density of functional human microvessels in the severe combined immunodeficient mouse model of human angiogenesis. [2] The combination of TW-37 and MEK inhibitors synergistically block melanoma cell growth in mice by a significant reduction in tumor volume and tumor mass. [3]
激酶实验 Fluorescence polarization-based binding assay for recombinant Bcl-2, Bcl-XL, and Mcl-1 protein : For this assay, the 21-residue BH3 peptide QEDIIRNIARHLAQVGDSMDR derived from Bid labeled with 6-carboxyfluorescein succinimidyl ester (FAM-Bid) and recombinant proteins derived from human Bcl-2,Bcl-X L,and Mcl-1 are employed. It is determined that FAM-Bid has a Ki of 11 nM to Bcl-2 protein,25 nM to Bcl-XL protein,and 5.7 nM to Mcl-1 protein. The competitive binding assay for Bcl-XL is same as that for Bcl-2 with the following exceptions: 30 nM Bcl-XL protein and 2.5 nM FAM-Bid peptide in the following assay buffer [50 mM Tris-Bis (pH 7.4) and 0.01% bovine gamma-globulin].
细胞实验 The sulforhodamine B (SRB) cytotoxicity assay is used as described. Briefly, optimal cell density for cytotoxicity assay is determined by growth curve analysis. HDMECs are seeded in a 96-well plate and allowed to adhere overnight. Drug or control is diluted in EGM2-MV and layered onto cells, which are allowed to incubate for times as indicated in the figures. Alternatively, HDMECs are coincubated with TW37 and 0 to 100 ng/mL recombinant human VEGF (rhVEGF)165 or 0 to 100 ng/mL recombinant human CXCL8. Cells are fixed on the plates by addition of cold trichloroacetic acid (10% final concentration) and incubation for 1 hour at 4 °C. Cellular protein is stained by addition of 0.4% SRB in 1% acetic acid and incubation at room temperature for 30 minutes. Unbound SRB is removed by washing with 1% acetic acid and the plates are air dried. Bound SRB is resolubilized in 10 mM unbuffered Tris-base and absorbance is determined on a microplate reader at 560 nm. Test results are normalized against initial plating density and drug-free controls. Data are obtained from triplicate wells per condition and are representative of at least three independent experiments(Only for Reference)
别名 TW 37
分子量 573.7
分子式 C33H35NO6S
CAS No. 877877-35-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 57.4 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7431 mL 8.7154 mL 17.4307 mL 43.5768 mL
5 mM 0.3486 mL 1.7431 mL 3.4861 mL 8.7154 mL
10 mM 0.1743 mL 0.8715 mL 1.7431 mL 4.3577 mL
20 mM 0.0872 mL 0.4358 mL 0.8715 mL 2.1788 mL
50 mM 0.0349 mL 0.1743 mL 0.3486 mL 0.8715 mL
100 mM 0.0174 mL 0.0872 mL 0.1743 mL 0.4358 mL

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TargetMol Library Books参考文献

1. Mohammad RM, et al. Clin Cancer Res, 2007, 13(7), 2226-2235. 2. Zeitlin BD, et al. Cancer Res, 2006, 66(17), 8698-8706. 3. Verhaegen M, et al. Cancer Res. 2006, 66(23), 11348-11359.
ent-11alpha-Hydroxy-15-oxokaur-16-en-19-oic acid Chelerythrine Medicarpin Cimidahurinine BDA-366 PROTAC Bcl2 degrader-1 Panaxynol 2-Hydroxychalcone

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 铜死亡化合物库 细胞凋亡化合物库 抗癌化合物库 已知活性化合物库 线粒体靶向库 抗衰老化合物库 PPI抑制剂库

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Keywords

TW-37 877877-35-5 Apoptosis BCL TW 37 TW37 inhibit Bcl-2 Family Inhibitor inhibitor

 

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