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SB-743921 HCl

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Chemical Structure| 940929-33-9 同义名 : SB-743921;SB-743921 (hydrochloride);SB-743921 hydrochloride
CAS号 : 940929-33-9
货号 : A654863
分子式 : C31H34Cl2N2O3
纯度 : 99%+
分子量 : 553.519
MDL号 : MFCD18385010
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(189.7 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 10 mg/mL(18.07 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • Kinesin

    KSP (P388 cells), IC50:14.4 nM

    KSP, Ki:0.07 nM
描述 SB-743921 is a second generation, highly potent and active KSP inhibitor with Ki of 0.1 nM, showing no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00136513 Solid Tumor Cancer Phase 1 Completed - United States, Pennsylvania ... 展开 >> GSK Investigational Site Pittsburgh, Pennsylvania, United States, 15232 United States, Wisconsin GSK Investigational Site Madison, Wisconsin, United States, 53792 收起 <<
NCT00343564 Non-Hodgkin's Lymphoma ... 展开 >> Hodgkin's Disease 收起 << Phase 1 Phase 2 Completed - United States, New Jersey ... 展开 >> Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, New York Cornell University Medical Center New York, New York, United States, 10021 Memorial Sloan-Kettering Caner Center New York, New York, United States, 10021 Herbert Irving Comprehensive Cancer Center New York, New York, United States, 10032 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Tennessee Sarah Cannon Cancer Research Institute Nashville, Tennessee, United States, 37203 Russian Federation Russian Medical Academy of Postgraduate Education Moscow, Russian Federation, 115478 St. Petersburg State PAVLOV Medical University Saint Petersburg, Russian Federation, 197002 收起 <<
NCT00343564 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.03mL

1.81mL

0.90mL

18.07mL

3.61mL

1.81mL
参考文献

[1]Holen KD, Belani CP, et al. A first in human study of SB-743921, a kinesin spindle protein inhibitor, to determine pharmacokinetics, biologic effects and establish a recommended phase II dose. Cancer Chemother Pharmacol. 2011 Feb;67(2):447-54.

[2]Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Jan-Feb;31(1):47-57.