1. Apoptosis
  2. MDM-2/p53
    Apoptosis
  3. COTI-2

COTI-2 

製品番号: HY-19896 純度: 99.40%
取扱説明書

COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.

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COTI-2 構造式

COTI-2 構造式

CAS 番号 : 1039455-84-9

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 99 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 90 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 160 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 235 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 350 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 600 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation[1][2][3].

IC50 & Target

p53[1]

体外実験

COTI-2 efficiently inhibits the proliferation rate 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). Relatively 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[2].

体内実験

COTI-2 significantly inhibits tumor growth in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. In addition to reducing tumor volumes at specific times post-treatment, COTI-2 also delays the time required for tumors to reach specified volumes. COTI-2 also significantly inhibits tumor growth in the SHP-77 SCLC xenograft model at a dose as low as 3 mg/kg. COTI-2 treatment both reduces U87-MG tumor volumes at specific times post-treatment and lengthens 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). COTI-2 treatment effectively inhibits OVCAR-3 xenograft growth regardless of the route of administration[2].

臨床実験
分子量

366.48

分子式

C₁₉H₂₂N₆S

CAS 番号

1039455-84-9

SMILES

S=C(N1CCN(C2=NC=CC=C2)CC1)N/N=C3CCCC4=C\3N=CC=C4

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 6.67 mg/mL (18.20 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7287 mL 13.6433 mL 27.2866 mL
5 mM 0.5457 mL 2.7287 mL 5.4573 mL
10 mM 0.2729 mL 1.3643 mL 2.7287 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.67 mg/mL (1.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
キナーゼ実験
[2]

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[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

細胞実験
[2]

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[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

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 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[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

COTI-2COTI2COTI 2MDM-2/p53Apoptosisanti-cancerlowtoxicityorallyHNSCCTNBCanti-proliferativeInhibitorinhibitorinhibit

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製品名:
COTI-2
製品番号:
HY-19896
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