RK-33
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
| Cell experiment:[1] | |
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Cell lines |
Various lung cancer cell lines |
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Reaction Conditions |
72 h incubation |
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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] | |
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Animal models |
Athymic NCr-nu/nu mice injected with A549 cells |
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Dosage form |
20 mg/kg Injected intraperitoneally |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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质量控制和MSDS
- 批次:
化学结构
