C188-9
(Synonyms: TTI-101) 目录号 : GC34076
A STAT3 inhibitor
Cas No.:432001-19-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
C188-9 is a STAT3 inhibitor.1,2 It binds to the phosphotyrosyl peptide binding site in the STAT3 Src homology 2 (SH2) domain (Ki = 136 nM) and inhibits G-CSF-induced activation of STAT3 in patient-derived acute myeloid leukemia (AML) cells (IC50s = 8-18 ?M). C188-9 induces apoptosis in patient-derived AML cells (EC50s = 6-50 ?M) and reduces viability of HepG2, Huh7, and PLC/PRF/5 hepatoma cells (IC50s = 10.19, 11.27, and 11.83 ?M, respectively).2,3 In vivo, C188-9 (100 mg/kg) reduces hepatic Pten deletion-induced hepatic macro- and microsteatosis, which reduces the development of hepatocellular carcinomas in mice. C188-9 (12.5 mg/kg) increases muscle fiber size in a murine Lewis lung carcinoma model of cancer cachexia.1
1.Silva, K.A.S., Dong, J., Dong, Y., et al.Inhibition of Stat3 activation suppresses caspase-3 and the ubiquitin-proteasome system, leading to preservation of muscle mass in cancer cachexiaJ. Biol. Chem.290(17)11177-11187(2015) 2.Redell, M.S., Ruiz, M.J., Alonzo, T.A., et al.Stat3 signaling in acute myeloid leukemia: Ligand-dependent and -independent activation and induction of apoptosis by a novel small-molecule Stat3 inhibitorBlood117(21)5701-5709(2011) 3.Jung, K.H., Yoo, W., Stevenson, H.L., et al.Multifunctional effects of a small-molecule STAT3 inhibitor on NASH and hepatocellular carcinoma in miceClin. Cancer Res.23(18)5537-5546(2017)
Cell experiment: | Cell lines are plated at 2 to 5×105 cells/mL in growth medium and treated with increasing doses of inhibitor for 24 hours. CD34+ AML cells are plated at 1 to 2×105 cells/mL in IMDM with 20% FBS and Pen/Strep, and incubated with C188-9 (0.3 to 100 μM) for 48 hours. Cells are then harvested and labeled. The fraction of spontaneous apoptosis is determined from an untreated sample and then subtracted from the drug-treated samples to yield the percentage of apoptosis attributed to drug treatment[1]. |
Animal experiment: | Mice[3]UM-SCC-17B cells (1.5×106) are injected into the tongues of athymic, 8-10 week old, male, nude mice. Once tumors are established, mice (20 total; 10/group) are randomized (average tumor vol ~15-20 mm3) to receive 5 times a week, intraperitoneal injections of either DMSO or C188 (50 mg/kg) or C188-9 (100 mg/kg). Tumor volumes are measured twice weekly. Average tumor volumes 6/πx (long dimension) x (short dimension)2)) are calculated and normalized to the volume at first day of treatment and plotted comparison is done by t test (* p<0.05) [3]. |
References: [1]. Silva KA, et al. Inhibition of Stat3 activation suppresses caspase-3 and the ubiquitin-proteasome system, leading to preservation of muscle mass in cancer cachexia. J Biol Chem. 2015 Apr 24;290(17):11177-87. | |
| Cas No. | 432001-19-9 | SDF | |
| 别名 | TTI-101 | ||
| Canonical SMILES | O=S(C1=CC=C(OC)C=C1)(NC2=C3C=CC=CC3=C(O)C(C4=C5C=CC=CC5=CC=C4O)=C2)=O | ||
| 分子式 | C27H21NO5S | 分子量 | 471.52 |
| 溶解度 | DMSO : ≥ 62 mg/mL (131.49 mM) | 储存条件 | 4°C, protect from light |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1208 mL | 10.604 mL | 21.208 mL |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2416 mL |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet