Filanesib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Filanesib is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.

Filanesib is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.(In Vitro):Filanesib shows anti-proliferative activity in multidrug-resistant cell lines including HCT-15, NCI/ADR-RES and K562/ADR with EC50 values of 3.7, 14 and 4.2 nM respectively. Filanesib (10 nM) blocks mitosis with the monopolar spindle structure typical of KSP inhibition as judged by both increased phosphorylation of histone H3 and the accumulation of cyclin B1 in four cells . Filanesib (1 nM) induces a significant G2M cell cycle block in OCI-AML3 cells at 24 hours .(In Vivo):Filanesib (10, 15, 20, 30 mg/kg, i.p.) is active in UISO-BCA-1 xenograft, and also superior to paclitaxel in mice bearing subcutaneous HT-29, HCT-116, MDA-MB-231 and A2780 xenografts. Filanesib is superior to docetaxel in the androgen receptor-negative prostate cancer xenograft model PC-3 . RPMI 8226 tumor xenografts are particularly sensitive to low doses of Filanesib (12.5 mg/kg, i.p.) . Filanesib significantly inhibits tumor growth in HL60 and MV4-11 xenografts of SCID mice at concentrations of 27 mg/kg and 20 mg/kg, respectively .

ARRY 520; ARRY-520

Others

Other Targets

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885060-09-3

420.5

C20H22F2N4O2S

>98% (HPLC)

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CN(C(=O)N1C(SC(=N1)C2=C(C=CC(=C2)F)F)(CCCN)C3=CC=CC=C3)OC

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(-20℃)

With Ice Pack

≥ 2 years