Tosedostat 托舍多特
CAS 238750-77-1 MFCD13185162
化学结构图
SMILES: CC(C)C[C@@H](C(=O)N[C@H](C(=O)OC1CCCC1)c1ccccc1)[C@H](O)C(=O)NO
化学属性
| Mol. Formula | C21H30N2O6 |
|---|---|
| Mol. Weight | 406.47 |
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | Tosedostat |
|---|---|
| CAS Number | 238750-77-1 |
| Synonym | (?S)-?-[[(2R)-2-[(1S)-1-Hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]amino]benzeneacetic Acid 2-(2-(hydroxy(hydroxycarbamoyl)methyl)-4-methylpentanoylamino)-2-phenylethanoic acid cyclopentyl ester CHR 2797 CHR-2797 CHR2797 CHR2797; CHR-2797; CHR 2797; Tosedostat. tosedostat |
| Chemical Name Translation | 托舍多特 |
| PubChem Substance ID | 15547703 |
| InChI | InChI=1S/C21H30N2O6/c1-13(2)12-16(18(24)20(26)23-28)19(25)22-17(14-8-4-3-5-9-14)21(27)29-15-10-6-7-11-15/h3-5,8-9,13,15-18,24,28H,6-7,10-12H2,1-2H3,(H,22,25)(H,23,26)/t16-,17+,18+/m1/s1 |
| LabNetwork Molecule ID | LN01303018 |
| Formula | C21H30N2O6 |
| IUPAC Name | (S)-cyclopentyl 2-((R)-2-((S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl)-4-methylpentanamido)-2-phenylacetate |
| InChIKey | FWFGIHPGRQZWIW-SQNIBIBYSA-N |
| Canonical SMILES | O=C(OC1CCCC1)[C@@H](NC([C@@H]([C@H](O)C(NO)=O)CC(C)C)=O)C2=CC=CC=C2 |
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分类
- Amines
- Aromatics
- Chiral Reagents
- Inhibitors
- Pharmaceuticals
- Intermediates & Fine Chemicals
产品应用
- Tosedostat is a proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death.
相关文献及参考
- [2]. Jenkins C, et al. Aminopeptidase inhibition by the novel agent CHR-2797 (tosedostat) for the therapy of acute myeloid leukemia. Leuk Res. 2011 May;35(5):677-81.
- [3]. Smith EM, et al. The combination of HDAC and aminopeptidase inhibitors is highly synergistic in myeloma and leads to disruption of the NFκB signalling pathway. Oncotarget. 2015 Jul 10;6(19):17314-27.
- Sato, Y., et al.: Biol. Pharm. Bull., 27, 772 (2004),
- [1]. Krige D, et al. CHR-2797: an antiproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells. Cancer Res. 2008 Aug 15;68(16):6669-79.
- [1]. Krige D, et al. CHR-2797: an antiproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells. Cancer Res. 2008 Aug 15;68(16):6669-79.
- [2]. Jenkins C, et al. Aminopeptidase inhibition by the novel agent CHR-2797 (tosedostat) for the therapy of acute myeloid leukemia. Leuk Res. 2011 May;35(5):677-81.
