产品说明
一般描述
A cell-permeable and irreversible bitter triterpenoid compound (NCI identifier: NSC 521777) that exhibits anti-proliferative and anti-tumor properties both in vitro and in vivo. Acts as a potent and highly selective inhibitor of Janus kinase/Signal transducer and activator of transcription 3 (Jak/STAT3) signaling pathway. Reported to suppress STAT3 tyrosine phosphorylation in v-src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells (IC50 = 500 nM), resulting in inhibition of STAT3 DNA-binding and STAT3-mediated gene transcription. Also shown to inhibit the growth of STAT3-transformed tumors in nude mice. Does not affect oncogenic pathways mediated by Ras, Akt1, ERK1/2, or JNK.
A cell-permeable and irreversible bitter triterpenoid compound (NCI identifier: NSC 521777) that displays anti-proliferative and antitumor properties both in vitro and in vivo. Acts as a potent and highly selective inhibitor of Janus kinase/signal transducer and activator of transcription 3 (JAK/STAT3) signaling pathway. It suppresses STAT3 tyrosine phosphorylation in v-Src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells (IC50 = 500 nM), resulting in inhibition of STAT3 DNA-binding and STAT3-mediated gene transcription. Shown to inhibit the growth of STAT3-transformed tumors in nude mice. Does not affect oncogenic pathways mediated by Ras, Akt, Erk1/2, or JNK.
包装
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
JAK/STAT3
Product does not compete with ATP.
Reversible: no
Target IC50: 500 nM suppressing STAT3 tyrosine phosphorylation in v-Src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells
警告
Toxicity: Standard Handling (A)
其他说明
Blaskovich, M.A., et al. 2003. Cancer Res.63, 1270.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C30H42O7 |
| 分子量 | 514.65 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white |
| 溶解性 | ethanol: 10 mg/mL DMSO: 100 mg/mL |
| 运输 | ambient |
| 储存温度 | −20℃ |
| InChI | 1S/C30H42O7/c1-25(2,36)12-11-21(33)30(8,37)23-19(32)14-27(5)20-10-9-16-17(13-18(31)24(35)26(16,3)4)29(20,7)22(34)15-28(23,27)6/h9,11-13,17,19-20,23,31-32,36-37H,10,14-15H2,1-8H3/b12-11+/t17-,19-,20+,23+,27+,28-,29+,30+/m1/s1 |
| InChI key | NISPVUDLMHQFRQ-MKIKIEMVSA-N |
安全信息
| 象形图 |  |
| 警示用语： | Danger |
| 危险声明 | H301 |
| 预防措施声明 | P264 - P270 - P301 + P310 - P405 - P501 |
| 危险分类 | Acute Tox. 3 Oral |
| 储存分类代码 | 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
