SB743921CAS号: 940929-33-9分子式: C31H33N2O3.HCl分子量: 553.52描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
SB-743921; SB 743921; SB743921
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外观 |
Powder
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可溶性/溶解性 |
DMSO 111 mg/mL (200.53 mM)
Ethanol 111 mg/mL (200.53 mM) Water 22 mg/mL (39.74 mM) |
生物活性 | |
靶点 |
KSP (MX1 cells),KSP (Colo205 cells),KSP,KSP (SKOV3 cells),KSP (MV522 cells),,
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In vitro(体外研究) |
The Ki of SB 743921 for human and mouse KSP is 0.1 nM and 0.12 nM, respectively, while the Ki of SB 743921 for other kinesins including MKLP1, Kin2 is more than 70 μM. SB 743921 blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death. SB-743921 has improved potency over ispinesib in both biochemical and cellular assays.
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In vivo(体内研究) |
SB-743921 is greater efficacy in vivo against P388 leukemia. SB-743921 has significant efficacy in a broad spectrum of tumor models differing from that of taxanes. SB-743921 is shown to have activity against advanced human tumor xenografts Colo205 (complete regressions), MCF-7, SK-MES, H69, OVCAR-3 (complete and partial regressions), and HT-29, MX-1, MDA-MB-231, A2780 (tumor growth delay). SB-743921 doesn’t cause the neuropathy often associated with the tubulin agents.
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分子结构图