Homoharringtonine CAS: 26833-87-4
MF: C29H39NO9
MW: 545.62
An inhibitor of diphenylalanine formation & acetylphenylalanyl-puromycin.

Homoharringtonine (CAS 26833-87-4)

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Noms alternatifs: Omacetaxine mepesuccinate; Cephalotaxine 4-methyl (2R)-2-hydroxy-2-(4-hydroxy-4-methylpentyl)butanedioate
Application: Homoharringtonine is an inhibitor of diphenylalanine formation & acetylphenylalanyl-puromycin
Numéro CAS: 26833-87-4
Pureté: ≥98%
Masse Moléculaire: 545.62
Formule Moléculaire: C29H39NO9
Information supplémentaire: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
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Homoharringtonine is a cephalotaxine alkaloid which inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes. Homoharringtonine has promising activity in hematologic malignancies and functions as an antileukemic. Homoharringtonine blocks the elongation phase of translation by binding to the 60-S ribosome subunit. Additionally, homoharringtonine has been shown to lower telomerase levels, inhibit protein synthesis, and induce apoptosis.


Références

1. Feldman, E., et al., 1992. Homoharringtonine is safe and effective for patients with acute myelogenous leukemia. Leukemia. 6(11): 1185-8. PMID: 1434802
2. Tujebajeva, R M., et al., 1992. Selective inhibition of the polypeptide chain elongation in eukaryotic cells. Biochimica et biophysica acta. 1129(2): 177-82. PMID: 1730056
3. Warrington, R C., et al., . Different effects of L-histidinol and homoharringtonine on 5-fluorouracil and bis-chloroethylnitrosourea activity in a murine model. Anticancer research. 11(5): 1879-83. PMID: 1768059
4. Kantarjian, H M., et al., 2001. Homoharringtonine: history, current research, and future direction. Cancer. 92(6): 1591-605. PMID: 11745238
5. Luo, Chang Ying., et al., 2004. Homoharringtonine: a new treatment option for myeloid leukemia. Hematology (Amsterdam, Netherlands). 9(4): 259-70. PMID: 15621733
6. Xie, Wan-Zhuo., et al., 2006. Homoharringtonine-induced apoptosis of human leukemia HL-60 cells is associated with down-regulation of telomerase. The American journal of Chinese medicine. 34(2): 233-44. PMID: 16552835

Apparence :
Powder
État Physique :
Solid
Dérivé de :
Cephalotaxus hainanensis
Solubilité :
Soluble in DMSO (100 mM), ethanol (50 mM), water (partly), chloroform, and methanol.
STOCKAGE :
Store at 4° C
Point de fusion :
143-145° C
Point d'Ébullition :
~713.1° C at 760 mmHg (Predicted)
Densité :
~1.3 g/cm3 (Predicted)
Indice de Réfraction :
n20D 1.61 (Predicted)
Activité Optique :
α20/D -125°, c = 0.25 in chloroform
IC50 :
KB: IC50 = 4 nM (human); A549: IC50 = 30 nM (human); P388: IC50 = 31.16 nM (mouse); Cytotoxicity against drug-resistant human KB-VIN cells: IC50 = 0.51 µM
Valeurs pK :
pKa: 11.6 (Predicted), pKb: 6.38 (Predicted)
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
WGK Allemagne :
3
RTECS :
FK0260000
PubChem CID :
Index Merck :
14: 10435
Numéro MDL :
MFCD03410264
Registre Beilstein :
5687925
SMILES :
CC(C)(CCC[[email protected]](CC(=O)OC)(C(=O)O[[email protected]]1[[email protected]]2C3=CC4=C(C=C3CCN5[[email protected]@]2(CCC5)C=C1OC)OCO4)O)O

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Homoharringtonine (CAS 26833-87-4)  Références bibliographiques

Consultez les publications faisant référence à l' utilisation de Homoharringtonine (CAS 26833-87-4). Cliquez sur le lien pour afficher lentrée PubMed .

Citations 1 à 8 sur un total de 8

PMID: # 29286665  Sakamoto, S.|Miyamoto, T.|Usui, K.|Tanaka, H.|Morimoto, S.| et al. 2018. J Nat Prod. 81: 34-40.

PMID: # 29344898  2018. Methods Mol. Biol. 1711: 351-398.

PMID: # 29490384  Pongkitwitoon, B.|Sakamoto, S.|Nagamitsu, R.|Putalun, W.|Tanaka, H.|Morimoto, S.| et al. 2018. Planta Med. 84: 1038-1044.

PMID: # 26762417  Chen, WL. et al. 2016. BMC Cancer. 16: 17.

PMID: # 25925126  Cell Commun Signal. 25.

PMID: # 31633216  Eur. J. Immunol. 49: 1457-1973.

PMID: # 27450084  Proc. Natl. Acad. Sci. U.S.A. 9015-20.

PMID: # 30205168  Cancer Lett. 197-218.

Citations 1 à 8 sur un total de 8
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