化學名

5-(benzylideneamino)-6-[(E)-benzylideneamino]-2-sulfanylidene-1H-pyrimidin-4-one

簡稱

SCR7

別名

CS-3903, AK174235, BC600700, QC-11823, X3557

中文名

N/A

化學式

C₁₈H₁₄N₄OS

分子量

334.4

CAS號

1533426-72-0

純度

98%

溶劑/溶解度

Water<1mg/ml; DMSO45mg/ml; Ethanol<1mg/ml

溶液配制

5mg加入1.5ml DMSO，或者每3.34mg加入1ml DMSO，配制成10mM溶液。SF1136-10mM用DMSO配制。

產品描述

SCR7 is a molecule that inhibits joining of DSBs in cell-free repair system; inhibits NHEJ (nonhomologous end-joining) in a Ligase IV-dependent manner within cells, and activates the intrinsic apoptotic pathway.

信號通路

Others

靶點

Ligase IV inhibitor

NHEJ inhibitor

－

－

－

IC50

~40nM

~40nM

－

－

－

體外研究

SCR7 does not induce DSBs directly to the genome and is Ligase IV dependent. Besides, upon incubation of oligomeric dsDNA or supercoiled plasmid DNA with increasing concentrations of SCR7, there was no evidence for DNA breaks. Accumulation of DSBs leads to cell death upon SCR7 treatment with a dose-dependent decrease in cell proliferation of MCF7, A549, and HeLa with an IC50 of 40, 34 and 44μM, respectively, which was further confirmed by DIC imaging in MCF7. T47D, A2780 and HT1080 were also sensitive to SCR7, with an IC50 of 8.5, 120, and 10μM, respectively. SCR7 encapsulated micelles (ES) were also characterized by small-angle neutron scattering (SANS). Encapsulated SCR7 treatment resulted in accumulation of DNA breaks within the cells, resulting in cell cycle arrest at G1 phase and activation of apoptosis.

體內研究

SCR7 treatment (10mg/kg, six doses) significantly reduced breast adenocarcinoma-induced tumor in mice. Untreated tumor animals survived only for 52 days, whereas treated animals exhibited ～4-fold increase in lifespan. Treatment with SCR7 resulted in regression of tumors with no obvious adverse effects. In addition, HPLC analysis of serum following administration of SCR7 into mice (20mg/kg) showed bioavailability of 114μg/ml and a t1/2 of 1hr.

臨床實驗

N/A

特征

N/A

酶活性檢測實驗

方法

N/A

細胞實驗

細胞系

N/A

濃度

N/A

處理時間

N/A

方法

N/A

動物實驗

動物模型

N/A

配制

N/A

劑量

N/A

給藥方式

N/A

產品編號

產品名稱

包裝

SF1136-10mM

SCR7 (DNA ligase IV抑制劑)

10mM×0.2ml

SF1136-5mg

SCR7 (DNA ligase IV抑制劑)

5mg

SF1136-25mg

SCR7 (DNA ligase IV抑制劑)

25mg

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說明書

1份