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[CAS NO. 885060-09-3] Filanesib
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-15187 |
| Brand: | MCE |
| CAS: | 885060-09-3 |
Overview
| MDL | MFCD18633235 |
|---|---|
| Molecular Weight | 420.48 |
| Molecular Formula | C20H22F2N4O2S |
| SMILES | O=C(N1[C@@](C2=CC=CC=C2)(CCCN)SC(C3=CC(F)=CC=C3F)=N1)N(OC)C |
3 Publications Citing Use of MCE
Summary
IC50 & Target
|
KSP 6 nM (IC 50 ) |
In Vitro
Filanesib induces mitotic arrest in multiple cell lines
[1]
.
Filanesib exhibits anti-proliferative against a broad range of human and rodent tumor cell lines, including a variety of leukemias and solid tumors, with EC
50
s between 0.4 nM and 14.4 nM
[1]
.
Filanesib (0.001-0.1 nM; 36 hours) induces apoptosis in a dose-dependent manner in HeLa cells
[1]
.
Filanesib (3.13-6.25 nM; 44 hours) causes accumulation of cells in the G2/M phase of the cell cycle in a dose-dependent manner in HeLa cells
[1]
.
Filanesib potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has potential to eradicate AML progenitor cells
[2]
.
Filanesib (3 μM; 6-24 hours) is able to induce caspase-2 activation
[3]
.
Filanesib (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [1]
| Cell Line: | Hela cells |
| Concentration: | 0.01-0.1 nM |
| Incubation Time: | 36 hours |
| Result: | Induced the formation of nucleosomes and activation of caspases-3 and 7. |
Cell Cycle Analysis [1]
| Cell Line: | HeLa cells |
| Concentration: | 0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM |
| Incubation Time: | 44 hours |
| Result: | Resulted in G2/M arrest. |
Western Blot Analysis [3]
| Cell Line: | Type II EOC cells |
| Concentration: | 3 μM |
| Incubation Time: | 6 hours, 12 hours, 24 hours |
| Result: | Induced caspase-2 activation in a time-dependent manner. |
Cell Cytotoxicity Assay [3]
| Cell Line: | Type II EOC cell lines (A2780, CP70, 01-28) |
| Concentration: | 0.003 μM, 0.03 μM, 0.3μM, 3 μM |
| Incubation Time: | 24 hours , 48 hours |
| Result: | Effectively decreased cell viability in a time-dependent manner in the Type II EOC cell lines. |
In Vivo
Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female nude mice, EOC mice xenograft model [3] |
| Dosage: | 20 mg/kg, 30 mg/kg |
| Administration: | Intraperitoneal injection, q4dx3 |
| Result: | Induced a decrease in tumor kinetics in a dose-dependent manner. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01372540 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
Plasma Cell Leukemia|Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma
|
February 24, 2012 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 237.82 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3782 mL | 11.8912 mL | 23.7823 mL |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 mL |
References
- [1] Christine Lemieux, et al. ARRY-520, a Novel, Highly Selective KSP Inhibitor with Potent Anti-Proliferative Activity. AACR Annual Meeting. 2007.
- [2] BZ Carter, et al. Inhibition of KSP by ARRY-520 Induces Cell Cycle Block and Cell Death via the Mitochondrial Pathway in AML Cells.
- [3] Ki Hyung Kim, et al. KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells. J Transl Med. 2009; 7: 63.
Synonyms
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