RubR1 Activator, GF-15 – Calbiochem

Descrição detalhada : A cell-permeable 2′-benzyloxy griseofulvin derivative that displays enhanced mammalian cancer-selective toxicity (IC50 ≤2, ≤4, ≤12, and ≥30 µM against panels of leukemia, myeloma, solid tumors, and non-malignant cell lines, respectively), but little antifungal activity, by activating spindle-assembly-checkpoint without affecting microtubule kinetochore attachment. Cancer cells are reported to undergo multipolar (MP) mitosis with normal or supernumerary centrosomes in the presence of GF-15, resulting in subsequent apoptotic cell death. Shown to retard HT29 colon cancer & OPM2 myeloma tumor expansion in mice (20 mg/kg/day i.p.) in vivo. GF-15 half-life is expected to be least 48 h in cultures.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable 2′-benzyloxy griseofulvin derivative that displays enhanced mammalian cancer-selective toxicity (IC50 ≤2, ≤4, ≤12, and ≥30 microM against panels of leukemia, myeloma, solid tumors, and non-malignant cell lines, respectively), but little antifungal activity, by activating spindle-assembly-checkpoint (Pos. vs. Neg. RubR1 staining of metaphase PC-3 kinetophores with or without 24 h 0.75 microM GF-15 treatment) without affecting microtubule kinetochore attachment (Neg. Mad2 staining of metaphase PC-3 kinetophores with or without GF-15). Cancer cells are reported to undergo multipolar (MP) mitosis with normal or supernumerary centrosomes (Aberrant vs. declustered, respectively) in the presence of GF-15 (%Declustered / %Aberrant MP mitotic cells among all anaphase cells = 5.6/<0.5, 10/3.9, 16/18, 28/30, respectively, in PC-3 cultures treated with 0, 0.375, 0.75, or 1.5 microM GF-15 for 24 h), resulting in subsequent apoptotic cell death. Shown to retard OPM2 myeloma- and HT29 colon cancer-derived tumor expansion in mice (by 49% and 56%, respectively at the end of 2-wk treatment; 10 i.p. dosages at 20 mg/kg/day in 2 weeks) in vivo. Based on stability data obtained with its p-iodobenzyl analogue, GF-15 half-life is expected to be least 48 h in cultures.
Sinónimos : RubR1 Activator, GF-15 - Calbiochem; Supernumerary Centrosomes Clustering Inhibitor, 2?-Benzyloxy-2?-demethoxygriseofulvin, (2 S,6? R)-(7-Chloro-4,6-dimethoxy-benzofuran-3-on)-2-spiro-1?-(2?-benzyloxy-6?-methylcyclohex-2?-en-4?-one), (2; Supernumerary Centrosomes Clustering Inhibitor, 2?-Benzyloxy-2?-demethoxygriseofulvin, (2S,6?R)-(7-Chloro-4,6-dimethoxy-benzofuran-3-on)-2-spiro-1?-(2?-benzyloxy-6?-methylcyclohex-2?-en-4?-one), (2S
Fórmula molecula r: C23H21ClO6
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X1EA