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CAS号:112522-64-2
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英文名称:CI-994
分子式
C15H15N3O2
分子量
269
EINECS号
200-256-5
MDL
MFCD00866266
Smiles
InChIKey
乙二醇化学百科
基本信息
物化性质
安全信息
生产及用途
CI994 (Tacedinaline)是一种抗癌药,抑制HDAC1,IC50为0.57 μM,使细胞周期停滞在G1期。Phase 3。CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells. CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. CI-994 exerts activity against several tumor cell lines with greater cytotoxicity against the solid tumors relative to both the leukemia and normal fibroblast cell lines. CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM.CI-994 exerts demonstrated antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP.Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) 是一种选择性的I型HDAC抑制剂,其对HDAC 1, 2, 3,和8的IC50分别为0.9, 0.9, 1.2, 和 >20 μM。Phase 3。
A-549和LX-1细胞中,CI-994(< 160 mM)表现出抑制细胞生长的作用,伴随G0/G1期增加,S期减少,且细胞凋亡增加。 CI-994抑制LNCaP细胞的生长,IC50为7.4 μM。 CI-994对几种肿瘤细胞系具有活性,相对于白血病和正常成纤维细胞系,对固体肿瘤具有更高的细胞毒性。 CI-994抑制大鼠白血病BCLO细胞的生长,IC50为2.5 μM。 CI-994对几种肿瘤模型,包括耐化疗的胰腺导管癌小鼠,和人前列腺肿瘤模型LNCaP,具有已证实的抗肿瘤活性。
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