ENMD-119
CAS 864668-87-1 MFCD64668871
化学结构图
SMILES: COc1cc2c(cc1C(N)=O)CCC1C2CC[C@]2(C)C=CCC12
化学属性
| Mol. Weight | 311.42 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | ENMD-1198 |
|---|---|
| Chemicalbook ID | CB82627803 |
| Formula | C20H25NO2 |
| Synonym | ENMD 1198; ENMD1198; ENMD 1198; IRC 110160; RC-110160; RC110160 |
| IUPAC Name | (13R)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15-octahydro-6H-cyclopenta[a]phenanthrene-3-carboxamide |
| InChIKey | YQJWOUQGXATDAE-CBTMWXCYSA-N |
| InChI | InChI=1S/C20H25NO2/c1-20-8-3-4-17(20)14-6-5-12-10-16(19(21)22)18(23-2)11-15(12)13(14)7-9-20/h3,8,10-11,13-14,17H,4-7,9H2,1-2H3,(H2,21,22)/t13?,14?,17?,20-/m0/s1 |
| Canonical SMILES | O=C(C1=C(OC)C=C2C3CC[C@]4(C)C=CCC4C3CCC2=C1)N |
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产品应用
- ENMD-1198 is a potent, orally-active, antimitotic agent that induces cell cycle arrest and apoptosis in tumor cells. ENMD-1198 has shown pronounced antitumor activity as well as substantial synergistic effects in combination with standard of care chemotherapeutic agents in numerous preclinical models. ENMD-1198 does not exhibit sensitivity to multi-drug resistance mechanisms in preclinical studies. ENMD-1198 also has shown preclinical activity towards taxane and vinca alkaloid resistant tumor cells. Additionally, ENMD-1198 decreases the activity of three oncogenic proteins (HIF-1α, NF-κB and STAT3) that are known to promote tumor growth and progression. ENMD-1198 has been evaluated in a Phase 1 clinical trial for safety, tolerability, pharmacokinetics, and clinical benefit in advanced cancer patients. (Source: http://www.entremed.com/science/enmd-1198/).
相关文献及参考
- [2]. Snoeks TJ, et al. 2-methoxyestradiol analogue ENMD-1198 reduces breast cancer-induced osteolysis and tumor burden both in vitro and in vivo. Mol Cancer Ther. 2011 May;10(5):874-82.
- [3]. Moser C, et al. ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma(HCC) cells, and inhibits growth and vascularization in vivo. BMC Cancer. 2008 Jul 23;8:206.
- [1]. Pasquier E, et al. ENMD-1198, a new analogue of 2-methoxyestradiol, displays both antiangiogenic and vascular-disrupting properties. Mol Cancer Ther. 2010 May;9(5):1408-18.
- [1]. Pasquier E, et al. ENMD-1198, a new analogue of 2-methoxyestradiol, displays both antiangiogenic and vascular-disrupting properties. Mol Cancer Ther. 2010 May;9(5):1408-18.
- [2]. Snoeks TJ, et al. 2-methoxyestradiol analogue ENMD-1198 reduces breast cancer-induced osteolysis and tumor burden both in vitro and in vivo. Mol Cancer Ther. 2011 May;10(5):874-82.
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