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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。
RK-33图片
CAS NO:1070773-09-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)428.44
FormulaC23H20N6O3
CAS No.1070773-09-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 85 mg/mL (198.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 3,7-dihydro-3,7-bis[(4-methoxyphenyl)methyl]-2H-diimidazo[4,5-d:4',5'-f][1,3]diazepin-2-one

InChi Key: COUMZXFUZDBRCZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H20N6O3/c1-31-17-7-3-15(4-8-17)11-28-14-26-19-20-22(25-13-24-21(19)28)29(23(30)27-20)12-16-5-9-18(32-2)10-6-16/h3-10,13-14H,11-12H2,1-2H3

SMILES Code: O=C1N(CC2=CC=C(OC)C=C2)C3=NC=NC4=C(N=CN4CC5=CC=C(OC)C=C5)C3=N1

Synonyms

RK-33; RK 33; RK33.

实验参考方法
In Vitro

In vitro activity: RK-33 binds specifically to DDX3, but not to the closely related proteins DDX5 and DDX17. RK-33 inhibits cancer growth and radiosensitizes lung cancer cells in a DDX3-dependent manner. RK-33 has no effect on either mitochondrial respiration or ATP generation. RK-33 curbs proliferation and induces apoptosis in a DDX3-dependent fashion. Wnt signaling is mediated by DDX3 and inhibited by RK-33. RK-33 impairs radiation-induced DNA damage repair by inhibiting NHEJ activity.


Cell Assay: Healthy, 60-70% confluent MDA-MB-231 cells are transduced with shDDX3 lentivirus particles. Knockdown of DDX3 expression is confirmed both by qRT-PCR and immunoblotting. MDA-MB-231 cells are treated with RK-33 (7.5 μM) for 12 h and harvested for RNA. Microarray experiments are performed.

In VivoRK-33 in combination with radiation induces tumor regression in multiple mouse models of lung cancer. RK-33, at the dose used, is non-toxic in SCID mice. RK-33-treated mice do not exhibit any discernable morphological changes.
Animal modelThe effect of RK-33 with a fractional dosing regimen was studied in the Twist1/KrasG12D lung cancer model. Results showed that during the 3 weeks treatment, a modest decrease in tumor growth with radiation and even more so with the combination of RK-33 and radiation. Therefore, these data indicated that RK-33 in combination with hypofractionated radiation was able to decrease lung tumor load effectively in preclinical lung cancer models and performed much better than the commonly used radiosensitizer carboplatin.
Formulation & DosageN/A
References

EMBO Mol Med. 2015 May;7(5):648-69.