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CX-4945 [Silmitasertib],≥99% (HPLC)

别名:5-[(3-氯苯基)氨基]-苯并[C]-2,6-萘啶-8-羧酸;5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid

CAS:1009820-21-6;分子式:C19H12ClN3O2;分子量:349.77;MDL:MFCD13184796
制造商品牌: BSZH 科学公司
货号(SKU): C06070
CAS号: 1009820-21-6
MDL号: MFCD13184796
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$244.16

产品描述

Application

一种选择性的有效的CK2(酪蛋白激酶2)抑制剂。

CX-4945 (Silmitasertib) is an ATP-competitive CK2 protein kinase inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad-spectrum anti-proliferative activity in multiple cancer cell lines. The anti-proliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 causes cell-cycle arrest and selectively induced apoptosis in certain cancer cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo. CX-4945 is an inhibitor of Flt-3/Flk-2 and Pim-1.

CX-4945(Silmitasertib)是一种具有ATP竞争性的CK2蛋白激酶抑制剂,对于重组人CK2α,Ki和IC50分别为0.38和1 nM。 CX-4945在多种癌细胞系中具有广谱抗增殖活性。 CX-4945对癌细胞的抗增殖活性与CK2α催化亚基的表达水平相关。 CX-4945使PI3K / Akt信号减弱,这是通过CK2特异性S129位点以及规范的S473和T308调控位点上Akt的去磷酸化来证明的。 CX-4945抑制Akt信号传导并抑制HUVEC细胞的增殖。 CX-4945导致细胞周期停滞并选择性诱导某些癌细胞的凋亡。在血管生成模型中,CX-4945抑制人脐静脉内皮细胞迁移,管形成,并阻断癌细胞中CK2依赖性缺氧诱导的因子1α(HIF-1α)的转录。集体地,CX-4945在体外和体内抑制促血管生成的CK2信号传导。 CX-4945是Flt-3 / Flk-2和Pim-1的抑制剂。

性质

Iupac Name5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid
Inchi Code1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25)
Inchi KeyMUOKSQABCJCOPU-UHFFFAOYSA-N


安全信息

个人防护装备 dust mask type N95 (US)EyeshieldsGloves
危害码 (欧洲) Xn
风险声明 (欧洲) 22
RIDADR NONH for all modes of transport
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16
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