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COTI-2
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。
COTI-2图片
CAS NO:1039455-84-9
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
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 366.48
Formula C19H22N6S
CAS No. 1039455-84-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: >70 mg/mL
Water: < 1 mg/mL
Ethanol: < 1 mg/mL
Chemical Name (E)-N'-(6,7-dihydroquinolin-8(5H)-ylidene)-4-(pyridin-2-yl)piperazine-1-carbothiohydrazide
Synonyms COTI2; COTI-2; COTI 2
SMILES Code S=C(N1CCN(C2=NC=CC=C2)CC1)N/N=C3CCCC4=C\3N=CC=C4
实验参考方法
In Vitro

In vitro activity: COTI-2 can potently inhibit the proliferation of all the tested cell lines following 72 h of treatment. COTI-2 is significantly effective at inhibiting tumor cell proliferation in all three cell lines (COLO-205, HCT-15, and SW620). Low concentrations of COTI-2 are active against all human glioblastoma cell lines tested (U87-MG, SNB-19, SF-268, and SF-295). COTI-2 treatment of SHP-77 cells with approximate IC50 concentrations results in the induction of early apoptosis among 40 to 47% of total cells.


Kinase Assay: The activity of COTI-2 against 227 kinases is tested using the AMBIT BIOSCIENCES KINOMESCAN assay. Briefly, streptavidin-coated magnetic beads are treated with biotinylated small molecule ligands for 30 min at 25°C to generate affinity resins for kinase assays. The liganded beads are blocked with excess biotin and washed with blocking buffer (1% BSA, 0.05% Tween 20, 1 mM DTT) to remove unbound ligand and to reduce non-specific binding. Binding reactions are assembled by combining phage lysates, liganded affinity beads, and COTI-2 in 1× binding buffer (20% SeaBlock, 0.17× PBS, 0.05% Tween 20, 6 mM DTT). All reactions are carried out in polystyrene 96-well plates that have been pre-treated with blocking buffer in a final volume of 0.1 mL.


Cell Assay: SHP-77 cells were treate with COTI-2 at various concentrations for 48 h. Cells were then washed twice with 1X cold PBS and stained with Annexin V and 7AAD. Briefly, 5 μl of Annexin V and 7AAD were added to 1 × 105 cells and incubated for 15 min at room temperature in the dark. Then 400 μl of the 1X binding buffer was added to the cells.

In VivoCOTI-2 suppressed tumor growth significantly in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. COTI-2 also significantly inhibited tumor growth in the SHP-77 SCLC xenograft model at a dose of as low as 3 mg/kg. The treatment by COTI-2 delays U87-MG, MDA-MB-231 and OVCAR-3 xenograft growth. COTI-2 treatment demonstrates a safe toxicity profile in vivo. COTI-2 selectively targets a wide variety of human cancer cell lines, as demonstrated by the in vitro data, while having little deleterious effects on normal cells.
Animal model mice
Formulation & Dosage Dissolved in saline; 10 mg/kg; i.p.
References Oncotarget. 2016 Jul 5; 7(27): 41363–41379.