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| 产地 | 中国 |
| 品牌 | Chemstan |
| 货号 | LC-01 |
| 用途 | 中间体 |
| 包装规格 | 20mg |
| 纯度 | 98%% |
| CAS编号 | 170364-57-5 |
| 是否进口 | 否 |
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| 常用名 | 恩扎妥林 | 英文名 | Enzastaurin |
|---|---|---|---|
| CAS号 | 170364-57-5 | 分子量 | 515.605 |
| 密度 | 1.34 | 沸点 | 767.2±60.0 °C at 760 mmHg |
| 分子式 | C32H29N5O2 | 熔点 | 249-261℃ |
| MSDS | 中文版 美版 | 闪点 | 417.8±32.9 °C |
Enzastaurin 是一种有效的 PKCβ 抑制剂，IC50 值为 6 nM；对其选择性是对 PKCα，PKCγ 和 PKCε 的 6-20 倍。
Fields of Application :
Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.
| CAS Number: | 170364-57-5 |
| Purity: | >98% |
| Molecular Weight: | 515.61 |
| Molecular Formula: | C32H29N5O2 |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione |
| Chemical Name: | |
| Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
Enzastaurin application results in a marked dose-dependent inhibition of growth in all MM cell lines investigated, including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266, with IC50 from 0.6-1.6 μM. Enzastaurin direct impacts human tumor cells, inducing apoptosis and suppressing proliferation in cultured tumor cells. Enzastaurin also suppresses the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308 while having no direct effect on VEGFR phosphorylation. Enzastaurin increases apoptosis in malignant lymphocytes of CTCL. When combined with GSK3 inhibitors, enzastaurin demonstrated an enhancement of cytotoxicity levels. Treatment with a combination of enzastaurin and the GSK3 inhibitor AR-A014418 led to increased levels of β-catenin total protein and β-catenin-mediated transcription. Blocking of β-catenin-mediated transcription or small hairpin RNA (shRNA) knockdown of β-catenin induced the same cytotoxic effects as that of enzastaurin plus AR-A014418. Additionally, treatment with enzastaurin and AR-A014418 decreased the mRNA levels and surface expression of CD44. Treatment of xenografts with Enzastaurin and radiation produced greater reductions in density of microvessels than either treatment alone. The decrease in microvessel density corresponded to delayed tumor growth. For the detailed information of Enzastaurin (LY317615), the solubility of Enzastaurin (LY317615) in water, the solubility of Enzastaurin (LY317615) in DMSO, the solubility of Enzastaurin (LY317615) in PBS buffer, the animal experiment (test) of Enzastaurin (LY317615), the cell expriment (test) of Enzastaurin (LY317615), the in vivo, in vitro and clinical trial test of Enzastaurin (LY317615), the EC50, IC50,and Affinity of Enzastaurin (LY317615), Please contact DC Chemicals.
