(R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of Filanesib (HY-15187). Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor with an IC50 of 6 nM.
分子量
420.48
Formula
C20H22F2N4O2S
CAS 号
885060-08-2
运输条件
Room temperature in continental US; may vary elsewhere.
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity[1].
IC50 & Target[1]
KSP
6 nM (IC50)
体外研究 (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 EC50s 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].
上海金畔生物科技有限公司 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.
体内研究 (In Vivo)
Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo[3].
上海金畔生物科技有限公司 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
分子量
420.48
Formula
C20H22F2N4O2S
CAS 号
885060-09-3
运输条件
Room temperature in continental US; may vary elsewhere.
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity[1].
IC50 & Target
IC50: 6 nM (KSP)[1]
体外研究 (In Vitro)
Filanesib TFA inhibits human KSP with an IC50 of 6 nM by a mechanism demonstrated to be uncompetitive with respect to ATP and noncompetitive with respect to tubulin[1]. Filanesib TFA induces mitotic arrest in multiple cell lines[1]. Filanesib TFA exhibits anti-proliferative against a broad range of human and rodent tumor cell lines[1]. Filanesib TFA (0.001-0.1 nM; 36 hours) induces apoptosis, by a mechanism that is independent of p53 status, as defined by formation of nucleosomes and activation of caspases 3 and 7, as well as accumulation in SubG0/1 by FACS [1]. Filanesib TFA (0.1-100 nM; 18 hours) induces the accumulation of phospho-Histone H3 (a marker of mitosis, and an indicator of mitotic arrest) in HeLa cells[1]. Filanesib TFA (0.78-6.25 nM; 44 hours) treatment results in G2/M arrest[1]. Filanesib TFA (10 nM; 16 hours) treatment results in the formation of monopolar spindles[1]. Filanesib TFA 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 TFA (3 μM; 6-24 hours) is able to induce caspase-2 activation[3]. Filanesib TFA (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells[3].
Shanghai Jinpan Biotech Co Ltd 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 cell death by apoptosis.
Cell Cycle Analysis[1]
Cell Line:
HeLa cells
Concentration:
44 hours
Incubation Time:
0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM
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.
体内研究 (In Vivo)
Filanesib TFA (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo[3].
Shanghai Jinpan Biotech Co Ltd 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
分子量
534.50
Formula
C22H23F5N4O4S
CAS 号
1781834-99-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[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.