BP-1-102
目录号 : GC34063
A STAT3 inhibitor
Cas No.:1334493-07-0
Sample solution is provided at 25 µL, 10mM.
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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)
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. | |
| Cas No. | 1334493-07-0 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO : ≥ 33 mg/mL (52.67 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5959 mL | 7.9797 mL | 15.9594 mL |
| 5 mM | 0.3192 mL | 1.5959 mL | 3.1919 mL |
| 10 mM | 0.1596 mL | 0.798 mL | 1.5959 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet