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COTI-2

Catalog No. T4325 CAS 1039455-84-9

Synonyms: COTI 2, COTI2

COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.

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COTI-2, CAS 1039455-84-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 105.00
25 mg	In stock	$ 193.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 490.00
500 mg	In stock	$ 1,090.00
1 mL * 10 mM (in DMSO)	In stock	$ 73.00

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Purity: 99.49%

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Description	COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.
In vitro	COTI-2 (72 h) potently inhibits the proliferation rate of all the tested cell lines. In COLO-205, HCT-15, and SW620 cell lines, COTI-2 markedly inhibits tumor cell proliferation. Relatively low concentrations of COTI-2 are active against all human glioblastoma cell lines tested (U87-MG, SNB-19, SF-268, and SF-295). In SHP-77 cells, COTI-2 treatment with IC50 concentrations causes the induction of early apoptosis among 40 to 47% of total cells.
In vivo	In the HT-29 human colorectal tumor xenografts, COTI-2 (10 mg/kg) markedly inhibits tumor growth. Except for reducing tumor volumes at specific times post-treatment, COTI-2 also increases the time required for tumors to reach specified volumes. In the SHP-77 SCLC xenograft model, COTI-2 (3 mg/kg) also markedly inhibits tumor growth. COTI-2 can reduce U87-MG tumor volumes at specific times post-treatment and lengthen the time required for U87-MG xenografts to grow in nude mice. Control tumors in mice treated with vehicle alone take only 5 days to reach an average volume of 828 mm3 while tumors in animals treated with COTI-2 take double that time (10 days) to reach a similar mean volume (857 mm3). Regardless of the route of administration, COTI-2 potently inhibits OVCAR-3 xenograft growth.
Kinase Assay	The interaction of COTI-2 with 227 kinases is tested using the AMBIT BIOSCIENCES KINOMESCAN assay. In brief, 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 Research	COTI-2 is dissolved in 100% dimethyl sulfoxide stock solution and diluted in medium plus FBS such that final DMSO concentrations are 0.5 to 1.0% depending on the experiment.SHP-77 cells are cultured with various concentrations of COTI-2 for 48 h. Cells are then washed twice with 1× cold PBS and stained with Annexin V and 7AAD according to the manufacturer's instructions. Briefly, 5 μL of Annexin V and 7AAD are added to 1×105 cells and incubated for 15 min at room temperature in the dark. Then 400 μL of the 1× binding buffer (100 mM HEPES, pH 7.4, 140 mM NaCl, 2.5 mM CaCl2) is added to the cells. Finally, cells are analyzed using a flow cytometer.
Animal Research	SHP-77 and HT-29 cells are injected in 50% matrigel into flanks of NCr-nu mice (2×106 cells per injection site) (n=5 mice per group). In the case of SHP-77 xenografts, treatment with COTI-2 begins prior to the appearance of palpable tumors. One day after injection of SHP-77 cells, animals receive 3 mg/kg of COTI-2 (once every two days, up to 38 days). Tumor sizes are estimated at 5, 10, 17, 24, and 38 days, by standard caliper measurements. In the case of HT-29 xenografts, the capacity of COTI-2 to suppress the growth of established tumors is assessed. HT-29 xenografts are allowed to grow to 200 mm3 before starting IP treatment with COTI-2 (10 mg/kg, 5 days a week for 7 weeks) or saline IP. Tumor growth is measured every 4 days by caliper measurement.

Synonyms	COTI 2, COTI2
Molecular Weight	366.48
Formula	C19H22N6S
CAS No.	1039455-84-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (13.64 mM)

References and Literature

1. Bykov VJN,etal.Targeting mutant p53 for efficient cancer therapy.Nat Rev Cancer. 2018 Feb;18(2):89-102. 2. Salim KY,etal.COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo.Oncotarget. 2016 Jul 5;7(27):41363-41379. 3. Duffy MJ, et al. Mutant p53 as a target for cancer treatment. Eur J Cancer. 2017 Sep;83:258-265.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Metabolism Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Lung Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

COTI-2 1039455-84-9 Apoptosis p53 COTI 2 inhibit Inhibitor HNSCC COTI2 low anti-cancer anti-proliferative toxicity TNBC MDM-2/p53 orally inhibitor

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