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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 | 1005342-46-0 |
| 是否进口 | 否 |
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Fields of Application :
LCL161 is an oral small molecule antagonist of Apoptosis Proteins (IAPs) that sensitizes a subset of tumors from diverse lineages to treatment with cytotoxic therapies.
| CAS Number: | 1005342-46-0 |
| Purity: | >98% |
| Molecular Weight: | 500.63 |
| Molecular Formula: | C26H33FN4O3S |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | LCL-161; LCL161 |
| Chemical Name: | (2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide |
| 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:
LCL161 is an oral small molecule antagonist of Apoptosis Proteins (IAPs) that sensitizes a subset of tumors from diverse lineages to treatment with cytotoxic therapies. in vitro: Huh-7 cells co-treated with LCL161 and SC-2001 showed a significant dose-dependent apoptotic effect demonstrated by sub-G1 assay and cleavage of PARP. Furthermore, the combination index (CI) ofLCL161 and SC-2001 showed a convincing synergism in resistant Huh-7. Results in human liver microsomes indicated LCL161 inhibited CYP3A in a concentration- and time-dependent manner (KI of 0.797 uM and kinact of 0.0803 min(-1) ). LCL161 activated human PXR in a reporter gene assay and induced CYP3A4 mRNA up to 5-fold in human hepatocytes. LCL161 caused rapid degradation of cIAP1 leading to TNFα secretion, LCL161 did not promote apoptosis significantly. However, LCL161 induced expression of MICA and MICB, ligands For the activating immune receptor NKG2D, and enhanced the susceptibility of HL cells to NKG2D-dependent lysis by NK cells. in vivo: The combinational therapy showed significant growth inhibition in Huh-7-bearing xenograft tumors. Notably, down regulation of Bcl-2 was observed in a tumor sample treated with LCL161 and SC-2001. Clinical trial: Phase I Trial of LCL-161 and Gemcitabine Plus Nab-Paclitaxel in Metastatic Pancreatic Cancer. Phase 1For the detailed information of LCL-161, the solubility of LCL-161 in water, the solubility of LCL-161 in DMSO, the solubility of LCL-161 in PBS buffer, the animal experiment (test) of LCL-161, the cell expriment (test) of LCL-161, the in vivo, in vitro and clinical trial test of LCL-161, the EC50, IC50,and Affinity of LCL-161.
References:
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