SB-743921 hydrochloride|940929-33-9|-陌孚医药/Medlife

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SB-743921 hydrochloride

目录号: PL14217 纯度: ≥99%

CAS No. :940929-33-9

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中文名称	SB-743921 hydrochloride
中文别名	(R)-n-(3-氨基丙基)-n-(1-(3-苄基-7-氯-4-氧代-4H-色烯-2-基)-2-甲基丙基)-4-甲基苯甲酰胺盐酸盐;N-(3-氨基丙基)-N-[(1R)-1-[7-氯-4-氧代-3-(苯基甲基)-4H-1-苯并吡喃-2-基]-2-甲基丙基]-4-甲基苯甲酰胺盐酸盐;SB743921 抑制剂;(R)-N-(3-氨基丙基)-N-(1-(3-苄基-7-氯-4-氧代-4H-苯并吡喃-2-基)-2-甲基丙基)-4-甲基苯甲酰胺盐酸盐
英文名称	SB-743921 hydrochloride
英文别名	SB 743921;(R)-N-(3-AMINOPROPYL)-N-(1-(3-BENZYL-7-CHLORO-4-OXO-4H-CHROMEN-2-YL)-2-METHYLPROPYL)-4-METHYLB...;Benzamide, N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methyl-, hydrochloride;SB 743921 hydrochloride;SB-743921;(R)-N-(3-AMINOPROPYL)-N-(1-(3-BENZYL-7-CHLORO-4-OXO-4H-CHROMEN-2-YL)-2-METHYLPROPYL)-4-METHYLBENZAMIDE HYDROCHLORIDE;N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methylbenzamide hydrochloride;SB743921;SB743921 HCl;C31H34Cl2N2O3;BCP02471;s2182;ABP000941;X7544;SW218123-2;SB743921 hydrochloride, >=98% (HPLC);N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methy;N-(3-Aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide;;SB-743921 hydrochloride;N-(3-Aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide;hydrochloride
Cas No.	940929-33-9
分子式	C₃₁H₃₄Cl₂N₂O₃
分子量	553.52
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

SB-743921 hydrochloride 是一种有效的驱动蛋白 (Eg5) 抑制剂，K_i 值为 0.1 nM。

生物活性

SB-743921 hydrochloride is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a K i of 0.1 nM.

性状

Solid

IC50 & Target[1][2]

Eg5 0.1 nM (Ki)

体外研究(In Vitro)

SB-743921 is a potent inhibitor of Eg5, with a Ki of 0.1 nM. SB-743921 (1 nM) potently inhibits colony forming cell (CFC) formation of chronic myeloid leukemia (CML) primary cells, but exhibits slight inhibitory activities on the colony-forming ability of normal bone marrow progenitors. SB-743921 (1, 3 nM) induces apoptosis of CML primary CD34 + cells, and shows slight effect on normal CD34 + cells. SB-743921 (2 nM) in combination with imatinib displays additive anti-proliferative effect in KCL22 and CML CD34 + cells. Furthermore, SB-743921 overcomes imatinib resistance in CML cells. SB-743921 (0.5 nM, 1 nM, 3 nM) inhibits MEK/ERK and AKT signaling in CML cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Jeffrey R. Jackson, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular Diagnostics in Cancer Therapeutic Development, Sep 12-15, 2006.
[2]. Yin Y, et al. Kinesin spindle protein inhibitor SB743921 induces mitotic arrest and apoptosis and overcomes imatinib resistance of chronic myeloid leukemia cells. Leuk Lymphoma. 2015 Jun;56(6):1813-20.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (180.66 mM)H₂O : 10 mg/mL (18.07 mM; ultrasonic and warming and heat to 60°C)

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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