BP-1-102

目录号: GC34063纯度: >98.50%

A STAT3 inhibitor


BP-1-102
Cas No.: 1334493-07-0
规格价格库存数量操作
2mg¥405.00现货
1
5mg¥635.00现货
1
10mg¥1,013.00现货
1
50mg¥4,050.00现货
1
100mg¥6,683.00现货
1
10mM (in 1mL DMSO)¥875.00现货
1

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产品描述 Description

BP-1-102 is an inhibitor of STAT3.1 It binds to STAT3 (Kd = 504 nM) and inhibits STAT3 binding to an IL-6R/gp130 peptide in a fluorescence polarization assay (IC50 = 4.1 μM). BP-1-102 (10-30 μM) decreases viability and proliferation of STAT3-dependent NIH3T3/v-Src, MDA-MB-231, PANC-1, DU145 and A549 cancer cells, but not STAT3-independent NIH3T3, NIH3T3/vRas, TE-71, and A2780S cancer cells. It reduces tumor growth and inhibits expression of the STAT3-dependent genes encoding c-Myc, survivin, Bcl-xL, cyclin D1, and VEGF in MDA-MB-231 and A549 mouse xenograft models when administered at doses of 1 and 3 mg/kg.

1.Zhang, X., Yue, P., Page, B.D., et al.Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenograftsProc. Natl. Acad. Sci. USA109(24)9623-9628(2012)

实验参考方法 Experimental Reference Method

Cell experiment:

Proliferating cells in 6- or 96-well plates are treated once with 0-30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a cell proliferation kit[1].

Animal experiment:

Mice: Athymic nude mice with established tumors are grouped and then given BP-1-102 (in 0.05% DMSO in water) at 1 or 3mg/kg (i.v.) every 2 or every 3 d or 3 mg/kg (oral gavage, 100 μL) every day for 15 or 20 d. Animals are monitored every day, and tumor sizes are measured with calipers and body weights are taken every 2 or 3 d. For each treatment group, the tumor volumes for each set of measurements are statistically analyzed in comparison with the control group using a paired T test[1].

References:

[1]. Zhang X, et al. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8.
[2]. De Simone V, et al. Th17-type cytokines, IL-6 and TNF-α synergistically activate STAT3 and NF-kB to promote colorectal cancer cell growth. Oncogene. 2015 Jul;34(27):3493-503.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
1334493-07-0
SMILES
O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1O
分子式
C29H27F5N2O6S
分子量
626.59 g/mol
溶解性
DMSO : ≥ 33 mg/mL (52.67 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol