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RTA 744

Names

[ CAS No. ]:
293736-67-1

[ Name ]:
RTA 744

[Synonym ]:
Berubicin HCl
WP744
RTA-744
Berubicin hydrochloride (USAN)

Biological Activity

[Description]:

RTA 744 (WP 744) is a Doxorubicin (HY-15142A) analogue. RTA 744 triggers apoptosis and cell killing in NB cells by activating proapoptotic mediators. RTA 744 has proapoptotic and anti-leukemia activities. RTA 744 can be used for cancer research[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer

[In Vitro]

WP 769 hydrochloride 抑制 K562 细胞的活性,IC50 值为 0.18 mg/mL[1]。 WP 769 hydrochloride (0-100 µM;24 h) 抑制 KBM-5 细胞吸收胸腺嘧啶[2]。 WP 769 hydrochloride (1 µM;15 min) 在 KBM-5 细胞中通过 NF-κB 的 p50 和 p65 亚基激活 NF-κB[2]。 WP 769 hydrochloride (0-100 µM;72 h) 以剂量依赖性方式抑制 Jurkat 和 RIP 缺失的 Jurkat 细胞增值[2]。 Cell Viability Assay[2] Cell Line: KBM-5 cells. Concentration: 0, 0.1, 1, 10 and 100 µM. Incubation Time: 24 h. Result: Inhibited cell viability with dose-dependent manner. Western Blot Analysis[2] Cell Line: KBM-5 cells. Concentration: 0, 0.1, 1 and 10 µM. Incubation Time: 4 h. Result: Increased NF-κB expression with time and dose dependent manner. Cell Viability Assay[3] Cell Line: SH-SY5Y cells. Concentration: 0.1, 1 and 10 µM. Incubation Time: 0, 1, 2, 3, 4 and 5 d. Result: Inhibited cell viability with dose-dependent manner. Apoptosis Analysis[3] Cell Line: SH-SY5Y cells. Concentration: 50, 500 and 2000 nM. Incubation Time: 48 h. Result: Promoted cell apoptosis. Western Blot Analysis[3] Cell Line: SH-SY5Y cells. Concentration: 0, 0.1, 1.0 or 10 µM. Incubation Time: 0, 0.5, 1, 2, 4, 6, 8, 12 or 24 h. Result: Activated Casp 3 and Casp 9. Increased p53 and NF-κB expression. Reduced IκBα expression.

[References]

[1]. Faderl S, et al. WP744, a novel anthracycline with enhanced proapoptotic and antileukemic activity. Anticancer Res. 2001 Nov-Dec;21(6A):3777-84.  

[2]. Ashikawa K, et al. Evidence that activation of nuclear factor-kappaB is essential for the cytotoxic effects of doxorubicin and its analogues. Biochem Pharmacol. 2004 Jan 15;67(2):353-64.  

[3]. Wu J, Harris NL, Inge TH. Nuclear factor-kappa B and apoptosis inducing factor activation by doxorubicin analog WP744 in SH-SY5Y neuroblastoma cells. J Surg Res. 2004 Dec;122(2):231-9.  

Chemical & Physical Properties

[ Molecular Formula ]:
C34H36ClNO11

[ Molecular Weight ]:
670.10300

[ Exact Mass ]:
669.19800

[ PSA ]:
195.07000

[ LogP ]:
3.72810


Related Compounds