618430-39-0

618430-39-0 structure
618430-39-0 structure
  • Name: SB-743291
  • Chemical Name: 24DSZ1VN92
  • CAS Number: 618430-39-0
  • Molecular Formula: C31H33ClN2O3
  • Molecular Weight: 517.058
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Kinesin
  • Create Date: 2018-07-04 04:05:57
  • Modify Date: 2025-08-27 09:27:15
  • SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases[1][2].

Name 24DSZ1VN92
Synonyms N-(3-Aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxo-4H-chromen-2-yl)-2-methylpropyl]-4-methylbenzamide
24DSZ1VN92
Benzamide, N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methyl-
Description SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases[1][2].
Related Catalog
In Vitro SB-743921 是一种有效的 Eg5 抑制剂,Ki 为 0.1 nM[1]。 SB-743921 (1 nM) 有效抑制慢性粒细胞白血病 (CML) 原代细胞的集落形成细胞 (CFC) 形成,但对正常骨髓祖细胞的集落形成能力表现出轻微的抑制活性[2]。 SB-743921 (1-3 nM) 诱导 CML 原代 CD34+ 细胞凋亡,对正常 CD34+ 细胞有轻微影响。 SB-743921 与伊马替尼联合使用,在 KCL22 和 CML CD34+ 细胞中表现出附加的抗增殖作用。 此外,SB-743921 克服了 CML 细胞对伊马替尼的耐药性[2]。 SB-743921(0.5 nM、1 nM、3 nM)抑制 CML 细胞中的 MEK/ERK 和 AKT 信号传导[2]。
In Vivo SB-743921 具有良好的口服生物利用度和药代动力学,可诱导携带肺癌患者异种移植物的裸鼠肿瘤完全消退[3]。
References

[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.  

[3]. Good JA, et al. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem. 2013 Mar 14;56(5):1878-93.  

Density 1.2±0.1 g/cm3
Boiling Point 683.0±55.0 °C at 760 mmHg
Molecular Formula C31H33ClN2O3
Molecular Weight 517.058
Flash Point 366.9±31.5 °C
Exact Mass 516.217957
LogP 6.79
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.613
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