RK-33

立即咨询

RK-33

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1070773-09-9

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
2mg	电议
5mg	电议
25mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	428.44
Cas No.	1070773-09-9
Formula	C₂₃H₂₀N₆O₃
Solubility	≥21.4 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name	3,7-bis(4-methoxybenzyl)-3,7-dihydro-2H-diimidazo[4,5-d:4',5'-f][1,3]diazepin-2-one
Canonical SMILES	COC1=CC=C(CN2C=NC3=C2N=CN=C(N4CC5=CC=C(OC)C=C5)C3=NC4=O)C=C1
运输条件	蓝冰运输或根据您的需求运输。
一般建议	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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

作用于具有高水平DDX3表达的癌细胞系（A549、H1299、H23和H460），IC50为4.4-8.4 μM。

RK-33是一种DDX3抑制剂。

已鉴定DDX3为一种RNA解旋酶，在多种癌症类型（例如肺癌）中过表达，并且与肺癌患者较低的存活相关。

体外：据报道，RK-33结合DDX3并消除其活性。在DDX3过表达细胞中，RK-33对 DDX3的抑制导致G1细胞周期停滞、诱导凋亡，并促进放射敏化。此外，由RK-33引起的DDX3功能丧失通过破坏DDX3-β-连环蛋白轴来削弱Wnt信号传导[1]。

体内：在Twist1 / KrasG12D肺癌模型中使用分次给药方案研究RK-33的作用。结果表明，在3周治疗期间，放射治疗引起肿瘤生长适度减少，并且RK-33和放射联合治疗肿瘤生长减少更多。因此，这些数据表明RK-33与低分光放射联合能够在临床前肺癌模型中有效地减少肺肿瘤负荷，并且比常用的放射增敏剂卡铂效果更好[1]。

临床试验：到目前为止，RK-33仍处于临床前研究阶段。

参考文献：
[1] Bol GM et al. Targeting DDX3 with a small molecule inhibitor for lung cancer therapy. EMBO Mol Med.2015 Mar 27;7(5):648-69.

试验操作

Cell experiment:[1]
Cell lines	Various lung cancer cell lines
Reaction Conditions	72 h incubation
Applications	Cancer cell lines with high levels of DDX3 expression (A549, H1299, H23, and H460) were more sensitive to RK-33 (IC50 = 4.4 ~ 8.4 μM) as compared to H3255, a cell line with low DDX3 expression (IC50 >25 μM). In addition, RK-33 also sensitized A549 cells to γ-radiation whilst it had no effect on the sensitivity of H3255 cells to γ-radiation. Therefore, RK-33 was able to inhibit cancer growth and radiosensitize lung cancer cells in a DDX3-dependent manner.
Animal experiment:[1]
Animal models	Athymic NCr-nu/nu mice injected with A549 cells
Dosage form	20 mg/kg Injected intraperitoneally
Applications	RK-33 significantly enhanced radiation-induced tumor regression in the orthotopic human lung cancer model. Hence, inhibition of DDX3 by RK-33 could be potentially utilized for lung cancer therapy.
Note	The technical data provided above is for reference only.
	References: 1. Bol GM, Vesuna F, Xie M, et al. Targeting DDX3 with a small molecule inhibitor for lung cancer therapy. EMBO Molecular Medicine, 2015, 7(5): 648-669.