5.00495
RubR1 Activator, GF-15
别名:
RubR1 Activator, GF-15, Supernumerary Centrosomes Clustering Inhibitor, 2ʹ-Benzyloxy-2ʹ-demethoxygriseofulvin, (2 S,6ʹ R)-(7-Chloro-4,6-dimethoxy-benzofuran-3-on)-2-spiro-1ʹ-(2ʹ-benzyloxy-6ʹ-methylcyclohex-2ʹ-en-4ʹ-one), (2, Supernumerary Centrosomes Clustering Inhibitor, 2ʹ-Benzyloxy-2ʹ-demethoxygriseofulvin, (2S,6ʹR)-(7-Chloro-4,6-dimethoxy-benzofuran-3-on)-2-spiro-1ʹ-(2ʹ-benzyloxy-6ʹ-methylcyclohex-2ʹ-en-4ʹ-one), (2S
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关于此项目
经验公式（希尔记法）:
C23H21ClO6
化学文摘社编号:
分子量:
428.86
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
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 (Pos. vs. Neg. RubR1 staining of metaphase PC-3 kinetophores with or without 24 h 0.75 µM 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 µM 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.
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Raab, M.S., et al. 2012. Cancer Res.72, 5374.
Ronnest, M.H., et al. 2009. J. Med. Chem.52, 3342.
Crosse, R., et al. 1964. J. Gen. Microbiol.34, 51.
Ronnest, M.H., et al. 2009. J. Med. Chem.52, 3342.
Crosse, R., et al. 1964. J. Gen. Microbiol.34, 51.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable